Rimonabant (SR141716)

中文名称：利莫那班

目录号：S3021 Purity: 99.67%

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

规格	价格	库存
10mM (1mL in DMSO)	990.19	现货
10mg	729.08	现货
25mg	1373.02	现货
50mg	2214.44	现货
100mg	3016.81	现货
1g	9990	现货
更大包装有超大折扣
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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 Otenabant (CP-945598) HCl 6-Iodopravadoline (AM630) GW842166X Org 27569	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

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(PMID)
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

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

ACAT1 ^[2]	ACAT2 ^[2]	MmpL3 ^[7]	hCB1 ^[1] (Cell-free assay)	hCB2 ^[1] (Cell-free assay)
			13.6 nM	1.64 μM

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]
激酶实验	配体结合试验
激酶实验	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。
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		29354056
	Immunofluorescence	β-catenin Lgr5		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]
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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
https://pubmed.ncbi.nlm.nih.gov/18802648/ https://pubmed.ncbi.nlm.nih.gov/20609360/ https://pubmed.ncbi.nlm.nih.gov/8070571/ https://pubmed.ncbi.nlm.nih.gov/19479993/ https://pubmed.ncbi.nlm.nih.gov/18469848/ https://pubmed.ncbi.nlm.nih.gov/17213845/ https://pubmed.ncbi.nlm.nih.gov/30682372/ + 展开

参考文献

https://pubmed.ncbi.nlm.nih.gov/18802648/
https://pubmed.ncbi.nlm.nih.gov/20609360/
https://pubmed.ncbi.nlm.nih.gov/8070571/

https://pubmed.ncbi.nlm.nih.gov/19479993/
https://pubmed.ncbi.nlm.nih.gov/18469848/
https://pubmed.ncbi.nlm.nih.gov/17213845/
https://pubmed.ncbi.nlm.nih.gov/30682372/

+ 展开

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

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

Ethanol : 30 mg/mL (64.68 mM)

DMSO : 26 mg/mL ( (56.05 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

DMSO : 25 mg/mL ( (53.9 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 2 mg/mL (4.31 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	5.000mg/ml (10.78mM)	以 1 mL 工作液为例，取50μL100mg/ml的澄清DMSO储备液加到400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入500μL ddH2O定容至 1 mL。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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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操作手册

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* 必填项

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Rimonabant (SR141716)

产品质控

Rimonabant (SR141716)相关产品

相关信号通路图

细胞实验数据示例

生物活性

化学信息&溶解度

实验计算

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