Rimonabant (SR141716)
中文名称：利莫那班
Rimonabant (SR141716)是一个大脑中心大麻素受体（CB1）特异性口服拮抗剂。在hCB1转染HEK293细胞中IC50浓度为13.6 nM，EC50浓度为17.3 nM。Rimonabant也是一种acyl CoA:cholesterol acyltransferases(ACAT) 1和2的双重抑制剂并且可抑制分支杆菌的MmpL3。
Rimonabant (SR141716) Chemical Structure
CAS: 168273-06-1
产品质控
批次：
纯度：
99.67%
99.67
Rimonabant (SR141716)相关产品
| 相关靶点 | CB1 CB2 | 点击展开 |
|---|---|---|
| 相关产品 | AM1241 AM251 BML-190 6-Iodopravadoline (AM630) 6-Iodopravadoline (AM630) Otenabant (CP-945598) HCl Org 27569 GW842166X | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I GPCR小分子化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| CHO | Function assay | > 0.1 nM | 1 hr | Inverse agonist activity at human recombinant CB1 receptor transfected in CHO cells assessed as reduction of [35S]GTPgammaS binding at > 0.1 nM after 1 hr by liquid scintillation spectrometry | 23357307 |
| N1E-115 | Function assay | 1 uM | 5 mins | Inverse agonist activity at CB1 receptor in mouse N1E-115 cells assessed as inhibition of WIN 55,212-2-induced ERK1/2 phosphorylation at 1 uM treated 5 mins prior to WIN 55,212-2 challenge by Western blot analysis | 23357307 |
| HEK293 | Function assay | 10 uM | Intrinsic activity at human recombinant CB1R expressed in HEK293 cells assessed as Eu-GTP binding at 10 uM relative to basal level | 19530697 | |
| CHOK1 | Function assay | 10 mins | Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay, Ki=0.0016μM | 19351113 | |
| CHO | Function assay | 60 mins | Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins, EC50=0.00011μM | 20047779 | |
| CHO | Function assay | 3 hrs | Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.00074μM | 20047779 | |
| CHO | Function assay | 10 mins | Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader, IC50=0.0032μM | 20047779 | |
| CHO | Function assay | 3 hrs | Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.126μM | 20047779 | |
| CHO-K1 | Function assay | 1 hr | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting, IC50=1.76μM | 20673729 | |
| CHO | Function assay | 1 hr | Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting, IC50=1.98μM | 21741835 | |
| HEK293 | Function assay | 5 mins | Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay, IC50=2.79μM | 21741835 | |
| CHO | Function assay | 90 mins | Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting, Ki=0.00073μM | 21962575 | |
| CHO | Function assay | 2 hrs | Displacement of [3H]CP55,940 from human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.0126μM | 22916707 | |
| CHO | Function assay | 2 hrs | Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.9μM | 22916707 | |
| CHO | Function assay | 1 hr | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cells incubated for 1 hr, Ki=0.0106μM | 23072339 | |
| HEK | Function assay | 1 hr | Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis, EC50=0.0015μM | 24175572 | |
| CHOK1 | Function assay | 1 hr | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHOK1 cells after 1 hr by liquid scintillation counting analysis, Ki=0.0059μM | 24175572 | |
| CHO | Function assay | 45 mins | Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=0.013μM | 24445310 | |
| CHO | Function assay | 45 mins | Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=9.8μM | 24445310 | |
| CHO-K1 | Function assay | 10 mins | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting, Ki=0.0016μM | 24900484 | |
| HEK293 | Function assay | 60 mins | Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting, Ki=0.0018μM | 24900484 | |
| CHO-K1 | Function assay | 60 mins | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting, Ki=0.522μM | 24900484 | |
| CHO | Function assay | 2 hrs | Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.0126μM | 24900561 | |
| CHO | Function assay | 2 hrs | Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.9μM | 24900561 | |
| CHO | Function assay | 90 mins | Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay, EC50=2.01μM | 24900561 | |
| Sf9 | Function assay | 20 mins | Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05μM | 25096297 | |
| Sf9 | Function assay | 20 mins | Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05012μM | 25096297 | |
| HEK293 | Function assay | 90 mins | Displacement of [3H]-CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.012μM | 26756097 | |
| HEK293 | Function assay | 90 mins | Displacement of [3H]-CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.79μM | 26756097 | |
| CHO | Function assay | 90 secs | Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay, EC50=0.005μM | 26827137 | |
| CHOK1 | Function assay | 90 mins | Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay, EC50=0.015μM | 29939744 | |
| HEK293 | Function assay | 90 secs | Inverse agonist activity at human CB1 receptor expressed in HEK293 cells co-expressing Galphaq16 assessed as inhibition of calcium mobilization after 90 secs by calcein-4 AAM dye-based FLIPR assay, EC50=0.586μM | 30077609 | |
| HEK293 | Function assay | 30 mins | Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay, EC50=0.0041μM | 30339387 | |
| CHO | Function assay | Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells, Kd=0.002512μM | 16140010 | ||
| CHO | Function assay | Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells, Ki=0.0054μM | 15801840 | ||
| CHO | Function assay | In vitro displacement of CP-55940 binding to human CB2 receptor expressed in CHO cells, Ki=1.58μM | 15771428 | ||
| CHO | Function assay | In vitro displacement of CP-55940 binding to human CB1 receptor expressed in CHO cells, Ki=0.025μM | 15771428 | ||
| CHO | Function assay | In vitro cannabinoid receptor 1 antagonism of [3H]arachidonic acid release by CHO cells, Kd=0.002512μM | 15771428 | ||
| CHO | Function assay | Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells, IC50=0.006μM | 15713403 | ||
| CHO | Function assay | Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells, Ki=1.58μM | 14736243 | ||
| CHO | Function assay | Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells, Ki=0.025μM | 14736243 | ||
| CHO | Function assay | Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells, Kd=0.002512μM | 14736243 | ||
| CHO cells | Function assay | Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes, Ki=8.9 nM | 10465552 | ||
| CHO | Function assay | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1, Ki=0.025μM | 16140010 | ||
| CHO | Function assay | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2, Ki=1.58μM | 16140010 | ||
| CHOK1 | Function assay | Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assay, Ki=0.001μM | 16263283 | ||
| HEK293 | Function assay | Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cells, Ki=0.0021μM | 16263283 | ||
| CHO | Function assay | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0054μM | 16279809 | ||
| HEK293 | Function assay | Displacement of [3H]SR-141716 from human CB1 receptor expressed in HEK293 cells, Kd=0.0018μM | 17004712 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0071μM | 17004712 | ||
| HEK293 | Function assay | Displacement of [3H]WIN-55212-2 from human CB1 receptor expressed in HEK293 cells, Ki=0.018μM | 17004712 | ||
| CHO | Function assay | Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells, IC50=0.0061μM | 17181138 | ||
| CHO | Function assay | Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells, IC50=0.6μM | 17181138 | ||
| CHO | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells, IC50=0.0061μM | 17293109 | ||
| CHO | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells, IC50=0.6033μM | 17293109 | ||
| HEK293 | Function assay | Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cells, Ki=0.0011μM | 17383180 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.016μM | 17942307 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=1.64μM | 17942307 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.047μM | 17979261 | ||
| CHOK1 | Function assay | Displacement of [3H]WIN-552122 from human recombinant CB2 receptor expressed in CHOK1 cells, Ki=1.99μM | 17979261 | ||
| HEK293 | Function assay | Displacement of radioligand from human CB1 receptor expressed in HEK293 cells, Ki=0.0018μM | 18083560 | ||
| HEK293 EBNA | Function assay | Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay, EC50=0.004μM | 18083560 | ||
| HEK293 | Function assay | Displacement of radioligand from human CB2 receptor expressed in HEK293 cells, Ki=0.554μM | 18083560 | ||
| CHOK1 | Function assay | Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay, IC50=0.12μM | 18243711 | ||
| CHOK1 | Function assay | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM | 18243711 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM | 18293908 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM | 18293908 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells, Ki=0.006μM | 18335976 | ||
| CHO | Function assay | Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells, IC50=1.76μM | 18337096 | ||
| CHO | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM | 18342403 | ||
| CHO | Function assay | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, Ki=1.58μM | 18342403 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0024μM | 18363352 | ||
| CHO | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=0.56μM | 18363352 | ||
| SF9 | Function assay | Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00031μM | 18448340 | ||
| SF9 | Function assay | Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00043μM | 18448340 | ||
| SF9 | Function assay | Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level, IC50=0.00135μM | 18448340 | ||
| SF9 | Function assay | Antagonist activity at human CB2 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.815μM | 18448340 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.04μM | 18511157 | ||
| CHO-K1 | Function assay | Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.00118μM | 18512901 | ||
| HEK293 | Function assay | Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated [35S]GTPgammaS binding, Kd=0.00257μM | 18512901 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM | 18512901 | ||
| CHO-K1 | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM | 18512901 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.008μM | 18579386 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM | 18579386 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.012μM | 18680276 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, Ki=0.79μM | 18680276 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM | 18712856 | ||
| HEK293 | Function assay | Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM | 18712856 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=1.9398μM | 18712856 | ||
| HEK293 | Function assay | Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as decrease in [35S]gammaGTP binding relative to control | 18712856 | ||
| CHO | Function assay | Antagonist activity at human CB1 receptor in CHO cells assessed as GTPgammaS binding, Kb=0.000698μM | 18800770 | ||
| CHOK1 | Function assay | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM | 18954042 | ||
| CHO | Function assay | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, IC50=1.76μM | 19022666 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=0.0019μM | 19095444 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM | 19095444 | ||
| HEK293 | Function assay | Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM | 19095444 | ||
| CHO-K1 | Function assay | Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay, Ki=0.00019μM | 19102698 | ||
| HEK293 | Function assay | Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells, Ki=0.0009μM | 19102698 | ||
| CHOK1 | Function assay | Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM | 19269817 | ||
| CHOK1 | Function assay | Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=0.24μM | 19328683 | ||
| CHOK1 | Function assay | Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=31.21μM | 19328683 | ||
| HEK293 | Function assay | Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.001995μM | 19338356 | ||
| HEK293 | Function assay | Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=0.39811μM | 19338356 | ||
| HEK293 | Function assay | Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.0019μM | 19520572 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells, IC50=0.0132μM | 19530697 | ||
| HEK293 | Function assay | Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding, EC50=0.0157μM | 19530697 | ||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells, IC50=1.6311μM | 19530697 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM | 19595596 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM | 19595596 | ||
| CHO-K1 | Function assay | Antagonist activity at human CB1 receptor transfected in CHO-K1cells by GTPgamma[35S] binding assay, Ki=0.0016μM | 19683918 | ||
| CHO | Function assay | Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.0925μM | 19850473 | ||
| CHOK1 | Function assay | Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM | 19850473 | ||
| CHO-K1 | Function assay | Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, IC50=0.0045μM | 19954978 | ||
| CHO-K1 | Function assay | Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay, IC50=0.0029μM | 20015647 | ||
| CHO-K1 | Function assay | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding, IC50=0.0045μM | 20015647 | ||
| COS7 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells, IC50=0.0051μM | 20015647 | ||
| CHO | Function assay | Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.108μM | 20045337 | ||
| CHO | Function assay | Antagonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release, Kd=0.002512μM | 20363132 | ||
| CHO | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM | 20363132 | ||
| CHO | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=1.58μM | 20363132 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells, Ki=0.012μM | 20718492 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells, Ki=0.79μM | 20718492 | ||
| CHO | Function assay | Agonist activity at human CB1 receptor expressed in CHO cells co-expressing Galpha16 protein assessed as mobilization of intracellular calcium, Ke=0.0011μM | 20845959 | ||
| HEK293 | Function assay | Displacement of [3H]SR141716 from human CB1 receptor expressed in HEK293 cells, Ki=0.00118μM | 20845959 | ||
| HEK293 | Function assay | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM | 20845959 | ||
| CHOK1 | Function assay | Displacement of [3H]CP55940 from human CB2 receptor expressed in CHOK1 cells, Ki=0.313μM | 20845959 | ||
| HEK | Function assay | Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells, Ki=0.012μM | 20943290 | ||
| HEK | Function assay | Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells, Ki=0.79μM | 20943290 | ||
| CHO | Function assay | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0009333μM | 21334892 | ||
| Sf9 | Function assay | Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in Sf9 cells, Ki=0.85114μM | 21334892 | ||
| CHO | Function assay | Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay, IC50=0.004μM | 21376588 | ||
| HEK293 | Function assay | Noncompetitive inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells by Dixon plot, Ki=1.4μM | 21511945 | ||
| HEK293 | Function assay | Noncompetitive inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells by Dixon plot, Ki=4μM | 21511945 | ||
| HEK293 | Function assay | Induction of MRP2-mediated E2-17betaG transport in human MRP2 expressing HEK293 cells in presence of 2 uM E2-17betaG | 21511945 | ||
| HEK293 | Function assay | Inhibition of MRP3-mediated E2-17betaG transport in human MRP3 expressing HEK293 cells in presence of 15 uM E2-17betaG | 21511945 | ||
| HEK293 | Function assay | Inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG | 21511945 | ||
| HEK293 | Function assay | Inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG | 21511945 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM | 21702498 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM | 21702498 | ||
| CHO-K1 | Function assay | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells co-expressing Galphaq16 assessed as inhibition of CP55940-induced intracellular calcium mobilization by fluorometry, Ke=0.0011μM | 22372835 | ||
| CHO-K1 | Function assay | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.0062μM | 22372835 | ||
| CHO-K1 | Function assay | Displacement of [3H]CP55940 from CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM | 22372835 | ||
| HEK | Function assay | Displacement of [3H]CP-55,940 from human recombinant CB1 receptor transfected in HEK cells, Ki=0.012μM | 22548457 | ||
| HEK | Function assay | Displacement of [3H]CP-55,940 from human recombinant CB2 receptor transfected in HEK cells, Ki=0.79μM | 22548457 | ||
| CHO | Function assay | Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level, IC50=0.051μM | 22959249 | ||
| CHO | Function assay | Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay, IC50=10.1μM | 23679955 | ||
| RD-HGA16 | Function assay | Antagonist activity at CB1-OX1 heterodimer (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of orexin A-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.001μM | 24944734 | ||
| RD-HGA16 | Function assay | Antagonist activity at CB1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of CP55940-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.0011μM | 24944734 | ||
| CHO | Function assay | Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=0.0135μM | 26151231 | ||
| CHO | Function assay | Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=9.1μM | 26151231 | ||
| HEK293 | Function assay | Immediate antagonist/Inverse agonist activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as reversal of 1 uM CP55,940-induced inhibition of 5 uM forskolin-induced cAMP accumulation by kinetic cAMP assay | 26203658 | ||
| CHO-K1 | Function assay | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940-induced intracellular calcium mobilization by Calcein-4 AM-staining based FLIPR assay, Ke=0.0011μM | 26827137 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| HEK293 | Function assay | Antagonist activity at human CB1 receptor expressed in HEK293 cells by GTPgammaS binding assay, Ke=0.0002μM | 30077609 | ||
| CHO | Function assay | Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay, Ki=0.143μM | 31609608 | ||
| CHO | Function assay | Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=2.01μM | ChEMBL | ||
| CHO | Function assay | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=10.1μM | ChEMBL | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Rimonabant (SR141716)是一个大脑中心大麻素受体（CB1）特异性口服拮抗剂。在hCB1转染HEK293细胞中IC50浓度为13.6 nM，EC50浓度为17.3 nM。Rimonabant也是一种acyl CoA:cholesterol acyltransferases(ACAT) 1和2的双重抑制剂并且可抑制分支杆菌的MmpL3。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | 有效诱导体重降低，并改善心血管代谢危险因素，然而由于引起严重的抑郁症和焦虑在2009年撤回。 | ||||||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Rimonabant剂量依赖性降低Raw264.7巨噬细胞和离体腹膜巨噬细胞中ACAT活性，IC50为2.9 μM。Rimonabant以近似的效能抑制完整CHO-ACAT1和CHO-ACAT2细胞以及无细胞试验中ACAT活性，对CHO-ACAT1和 CHO-ACAT2的IC50分别为1.5 μM和2.2 μM。与ACAT抑制一致，Rimonabant治疗阻断巨噬细胞中ACAT相关过程，氧甾醇诱导的细胞凋亡和乙酰化LDL诱导的泡沫细胞形成。[2] Rimonabant显著减少细胞生长，并诱导人结肠直肠癌细胞(DLD-1，CaCo-2和SW620)的死亡。Rimonabant能够改变所有测试细胞系中细胞周期分布。特别是，Rimonabant引起DLD-1细胞中细胞周期阻滞，而不诱导细胞凋亡或坏死。[4] |
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|---|---|---|---|---|
| 激酶实验 | 配体结合试验 | |||
| 将人CB1和CB2稳定转染的HEK 293细胞和细胞膜纯化。0.2-8 μg纯化的细胞膜与0.75 nM [3H] CP55,940和Rimonabant在孵育液(50 mM Tris-HCl，5 mM MgCl2，1 mM EDTA，0.3%BSA，pH 7.4)中培育。非特异性结合在1 μM CP55,940存在下定义。反应在30 °C下，Multiscreen中培育1.5小时。反应通过多重过滤终止，并且用冰预冷的洗涤缓冲液(50mM Tris，pH 7.4，0.25% BSA)清洗4次。过滤器上的放射性结合通过Topcount测量。IC50定义为抑制50%[3H] CP55,940结合时Rimonabant的浓度，并通过非线性回归计算。 | ||||
| 细胞实验 | 细胞系 | Raw 264.7细胞 | ||
| 浓度 | 0,1,4 μM | |||
| 孵育时间 | 17小时 | |||
| 方法 | Raw 264.7细胞(2×106/孔)在12孔板中用PBS漂洗，培养基用不同量Rimonabant增补，1小时后用7-酮基胆固醇(7KC)增补。所有孔加入等量的载体。培育16小时后，caspase-3和caspase 3样活性使用荧光底物(Ac-DEVD-AFC)和配备酶标仪的分光光度计测定。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | CD44 / Lgr5 / CD133 / EpCAM β-catenin p-LRP6 / LRP6 / Lgr5 |
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29354056 | |
| Immunofluorescence | β-catenin Lgr5 |
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29354056 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Rimonabant腹腔内给药或口服给药有效且剂量依赖性拮抗大麻素受体激动剂的经典药理学和行为作用。[3]在氧化偶氮甲烷诱发的结肠癌模型中，结肠直肠癌发生之前，Rimonabant显著减少异常隐窝病灶(ACF)的形成。[4] Rimonabant (10 mg/kg，强饲)对3个月大雄性肥胖Zucker大鼠喂食2周作为葡萄糖耐量降低模型，对6个月大雄性肥胖Zucker大鼠喂食10周作为代谢综合征模型。相对于瘦的Zucker大鼠，RANTES (正常T细胞表达和分泌的活性调节蛋白)和MCP-1 (单核细胞趋化蛋白-1)血清水平在肥胖Zucker大鼠体内增加，而在Rimonabant长期治疗下显著降低，这表明代谢综合征大鼠的体重增加。相对于瘦的Zucker大鼠，Neutrophils和单核细胞在年老和幼小的肥胖Zucker大鼠中显著增加，但是被Rimonabant降低。相对于瘦的Zucker大鼠，血小板结合的纤维蛋白原在两个年龄段肥胖Zucker大鼠中显著增加，但是被Rimonabant减少。来自肥胖大鼠的血小板对凝血酶诱导的聚集更敏感，并粘附在纤维蛋白原上，这都会被Rimonabant治疗减弱。[5] |
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|---|---|---|
| 动物实验 | Animal Models | 雄性小鼠和雄性大鼠 |
| Dosages | 20 ml/kg (小鼠) 和 5 ml/kg (大鼠) | |
| Administration | WIN55212-2静脉注射之前，Rimonabant 通过腹腔注射(30 分钟)或口服(1 小时)给药 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00750347 | Completed | Pain |
University Hospital Clermont-Ferrand |
September 2008 | Phase 1 |
| NCT00656487 | Completed | Cannabis Dependence|Cannabis Withdrawal |
The Scripps Research Institute|National Institute on Drug Abuse (NIDA) |
April 30 2008 | Phase 2 |
| NCT00546325 | Completed | Diabetes Mellitus Type 2 |
Sanofi |
October 2007 | Phase 3 |
| NCT00525681 | Completed | Renal Transplantation |
University of Oslo School of Pharmacy |
September 2007 | Phase 4 |
| NCT00584389 | Terminated | Obesity |
University of Surrey|European Foundation for the Study of Diabetes|Royal Surrey County Hospital NHS Foundation Trust |
July 2007 | Phase 4 |
| NCT01041170 | Completed | Cannabis|Dependence |
National Institute on Drug Abuse (NIDA)|National Institutes of Health Clinical Center (CC) |
April 16 2006 | Phase 1 |
化学信息&溶解度
| 分子量 | 463.79 | 分子式 | C22H21Cl3N4O |
| CAS号 | 168273-06-1 | SDF | Download Rimonabant (SR141716) SDF |
| Smiles | CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 92 mg/mL ( (198.36 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 50 mg/mL (107.8 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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