Nelfinavir Mesylate
别名: AG 1343 Mesylate 中文名称：甲磺酸奈非那韦
Nelfinavir Mesylate是强效的HIV protease抑制剂，Ki为2 nM。
Nelfinavir Mesylate Chemical Structure
CAS: 159989-65-8
产品质控
批次：
纯度：
99.51%
99.51
Nelfinavir Mesylate相关产品
| 相关靶点 | HIV-1 capsid HIV-1 caspid | 点击展开 |
|---|---|---|
| 相关产品 | Pepstatin A Limonin Temsavir (BMS-626529) | 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 蛋白酶抑制剂库 泛素化化合物库 | 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 |
|---|---|---|---|---|---|
| 12D7 | Antiviral assay | 0.08 to 1.25 uM | 3 days | Antiviral activity against HIV1 LAI infected in human 12D7 cells overexpressing p-gp assessed as reduction in P24 level at 0.08 to 1.25 uM incubated for 3 days followed by replacement of fresh medium containing compound and measured after 3 days by ELISA | 31505928 |
| HEK293 | Function assay | 0.12 uM | Inhibition of HIV1 NL4-3 proteins incorporation into virions transfected in HEK293 cells assessed as unprocessed gp160 Env protein at 0.12 uM by Western blot | 17646410 | |
| HEK293 | Function assay | 0.12 uM | Inhibition of HIV1 NL4-3 proteins incorporation into virions transfected in HEK293 cells assessed as aberrant Env protein at 0.12 uM by Western blot | 17646410 | |
| MDR1 | Function assay | 20 uM | Decrease in P-glycoprotein-mediated tenofovir disoproxil fumarate efflux in MDCK2 expressing human MDR1 cells at 20 uM | 17664327 | |
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E, EC50=0.011μM. | 18955518 | |
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA, EC50=0.17μM. | 18955518 | |
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA, EC50=0.21μM. | 18955518 | |
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA, EC50=0.24μM. | 18955518 | |
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA, EC50=0.32μM. | 18955518 | |
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA, EC50=0.51μM. | 18955518 | |
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA, EC50=0.65μM. | 18955518 | |
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay, EC50=0.22μM. | 20439612 | |
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay, EC50=0.29μM. | 20439612 | |
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay, EC50=0.3μM. | 20439612 | |
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay, EC50=0.32μM. | 20439612 | |
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay, EC50=0.37μM. | 20439612 | |
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay, EC50=0.51μM. | 20439612 | |
| CEM-SS | Antiviral assay | 6 days | Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay, ED50=0.03μM. | 15217281 | |
| HOG.R5 | Antiviral assay | 4 days | Antiviral activity against HIV1 3B infected in human HOG.R5 cells after 4 days, IC50=0.09μM. | 15217281 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=0.018μM. | 17576848 | |
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=0.048μM. | 17576848 | |
| CEM | Antiviral assay | 7 days | Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.1μM. | 17576848 | |
| CEM | Antiviral assay | 7 days | Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.177μM. | 17576848 | |
| CEM | Antiviral assay | 7 days | Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.199μM. | 17576848 | |
| CEM | Antiviral assay | 7 days | Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.281μM. | 17576848 | |
| HEK293 | Antiviral assay | 48 hrs | Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay, EC50=0.0058μM. | 17638694 | |
| MT4 | Antiviral assay | 6 days | Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay, EC50=0.029μM. | 17638694 | |
| MT4 | Cytotoxicity assay | 6 days | Cytotoxicity against human MT4 cells after 6 days by MTT assay, CC50=8μM. | 17638694 | |
| CEM-SS | Antiviral assay | 5 days | Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as reverse transcriptase activity after 5 days by MTT assay, IC50=0.002μM. | 17950955 | |
| MOLT-4/3B | Antiviral assay | 4 days | Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay, EC50=0.029μM. | 18316521 | |
| MT2 | Antiviral assay | 7 days | Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay, EC50=0.023μM. | 18955518 | |
| HeLa | Antiviral assay | 72 hrs | Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.013μM. | 19805571 | |
| HeLa | Antiviral assay | 72 hrs | Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.016μM. | 19805571 | |
| HeLa | Antiviral assay | 72 hrs | Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.038μM. | 19805571 | |
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against wild type HIV1 subtype C infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.00167μM. | 20404123 | |
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against wild type HIV1 subtype CRF02_AG infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.0057μM. | 20404123 | |
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against wild type HIV1 subtype B infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.0098μM. | 20404123 | |
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position and M46 mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.055μM. | 20404123 | |
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype CRF02_AG harboring protease L33I, M46I, A71T mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporte, EC50=0.202μM. | 20404123 | |
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype C harboring protease L23I, M46I, L89T mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene , EC50=0.272μM. | 20404123 | |
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype B harboring protease D30N, M46I, A71T and V77I mutant gene and polymorphism at M36 position of protease infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luci, EC50=1.139μM. | 20404123 | |
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype B harboring protease D30N, L33I, M46I, N88D mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter, EC50=1.463μM. | 20404123 | |
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype C harboring protease D30N, E35G, I85V, L90M mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter, EC50=3.473μM. | 20404123 | |
| TZM-bl | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype B harboring protease polymorphism at M36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 20404123 | |
| TZM-bl | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 20404123 | |
| TZM-bl | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype B harboring protease polymorphism at I36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 20404123 | |
| BESM | Antitrypanosomal assay | 88 hrs | Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50=12μM. | 20547819 | |
| BESM | Cytotoxicity assay | 88 hrs | Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50=32μM. | 20547819 | |
| CMEC/D3 | Function assay | 30 mins | Inhibition of P-gp in human CMEC/D3 cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis, IC50=1.7μM. | 31505928 | |
| CMEC/D3 | Function assay | 30 mins | Inhibition of P-gp in human CMEC/D3 cells using calcein-AM as substrate after 30 mins by flow cytometric analysis, IC50=2μM. | 31505928 | |
| 12D7-MDR | Function assay | 30 mins | Inhibition of P-gp in human 12D7-MDR cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis, IC50=5.8μM. | 31505928 | |
| 12D7-MDR | Function assay | 30 mins | Inhibition of P-gp in human 12D7-MDR cells using calcein-AM as substrate after 30 mins by flow cytometric analysis, IC50=9.1μM. | 31505928 | |
| 12D7 | Antiviral assay | 3 days | Antiviral activity against HIV1 LAI infected in human 12D7 cells overexpressing p-gp assessed as reduction in P24 level at 1:1 ratio of test compound to abacavir incubated for 3 days followed by followed by replacement of fresh medium containing compound | 31505928 | |
| MT2 | Antiviral assay | 5 days | Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay, EC50=0.0049μM. | ChEMBL | |
| HepG2 | Cytotoxicity assay | 5 days | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay, CC50=7.4μM. | ChEMBL | |
| skeletal myoblast cells | Cytotoxicity assay | 72 hours | DNDI: Cytotoxicity in Vitro, 72 hour, in rat skeletal myoblast cells, IC50=12.05μM. | ChEMBL | |
| MT2 | Cytotoxicity assay | 5 days | Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay, CC50=19.1μM. | ChEMBL | |
| HeLa | Function assay | TP_TRANSPORTER: inhibition of TEA uptake (TEA: 10 uM) in OCT1-expressing HeLa cells, IC50=21.8μM. | 10681378 | ||
| Caco-2 | Function assay | TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 5 uM) in Caco-2 cells, IC50=1.4μM. | 10820137 | ||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against Wild type virus in MT-4 cells, ED50=0.02μM. | 11543677 | ||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with compound 1), ED50=0.07μM. | 11543677 | ||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with ritonavir), ED50=0.11μM. | 11543677 | ||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with saquinavir), ED50=0.12μM. | 11543677 | ||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with nelfinavir), ED50=2.44μM. | 11543677 | ||
| LLC-PK1 | Function assay | Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=2.3μM. | 12699389 | ||
| LLC-PK1 | Function assay | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells, IC50=2.3μM. | 12699389 | ||
| LLC-PK1 | Function assay | Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=3.4μM. | 12699389 | ||
| LLC-PK1 | Function assay | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells, IC50=3.4μM. | 12699389 | ||
| HEK | Function assay | TP_TRANSPORTER: increase in mitoxantrone intracellular accumulation in BCRP-expressing HEK cells, IC50=12.5μM. | 15007102 | ||
| MT-4 | Function assay | Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells, ED50=0.02μM. | 15537350 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 HXB2 in MT4 cells, IC50=0.32μM. | 16458505 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 EP13 in MT4 cells, IC50=0.45μM. | 16458505 | ||
| PHA-PBMC | Antiviral assay | Antiviral activity against HIV1 BA-L isolate in human PHA-PBMC cells, IC50=0.007μM. | 16913714 | ||
| MT2 | Antiviral assay | Antiviral activity against HIV1 LAI isolate in human MT2 cells, IC50=0.01μM. | 16913714 | ||
| PHA-PBMC | Antiviral assay | Antiviral activity against HIV1 LAI isolate in human PHA-PBMC cells, IC50=0.014μM. | 16913714 | ||
| MT2 | Antiviral assay | Antiviral activity against HIV2 EHO isolate in human MT2 cells, IC50=0.02μM. | 16913714 | ||
| PHA-PBMC | Antiviral assay | Antiviral activity against multi drug-resistant HIV1 ET variant in human PHA-PBMC cells, IC50=0.032μM. | 16913714 | ||
| PHA-PBMC | Antiviral assay | Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells, IC50=0.17μM. | 16913714 | ||
| PHA-PBMC | Antiviral assay | Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells, IC50=0.31μM. | 16913714 | ||
| MT2 | Antiviral assay | Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.03μM. | 17371811 | ||
| MT2 | Antiviral assay | Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.032μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay, EC50=0.033μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.08μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.21μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.22μM. | 17371811 | ||
| MT2 | Antiviral assay | Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.24μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.27μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.27μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.34μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.47μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.48μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.49μM. | 17371811 | ||
| MT2 | Cytotoxicity assay | Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, CC50=8.1μM. | 17371811 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B in MT4 cells by MTT assay, EC50=0.016μM. | 17537628 | ||
| MT4 | Cytotoxicity assay | Cytotoxicity against MT4 cells by MTT assay, LC50=11μM. | 17537628 | ||
| MDCK2 | Inhibition of human | Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells, IC50=19.9μM. | 17664327 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT method, EC50=0.016μM. | 18426195 | ||
| MT4 | Cytotoxicity assay | Cytotoxicity against human MT4 cells by MTT assay, CC50=11μM. | 18426195 | ||
| MT4 | Antiretroviral assay | Antiretroviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.023μM. | 18541726 | ||
| MT4 | Antiretroviral assay | Antiretroviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.028μM. | 18541726 | ||
| MT4 | Antiviral assay | Antiviral activity against Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.029μM. | 18541726 | ||
| MT4 | Antiviral assay | Antiviral activity against non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.035μM. | 18541726 | ||
| MT4 | Antiretroviral assay | Antiretroviral activity against Human immunodeficiency virus 2 EHO infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.049μM. | 18541726 | ||
| MT4 | Antiretroviral assay | Antiretroviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.05μM. | 18541726 | ||
| MT4 | Antiretroviral assay | Antiretroviral activity against Simian immunodeficiency virus MAC 251 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.05μM. | 18541726 | ||
| MT4 | Antiviral assay | Antiviral activity against Protease inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.17μM. | 18541726 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA, EC50=0.018μM. | 18955518 | ||
| MT4 | Antiviral assay | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay, EC50=0.045μM. | 20439612 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay, EC50=0.13μM. | 20439612 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Nelfinavir Mesylate是强效的HIV protease抑制剂，Ki为2 nM。 | ||
|---|---|---|---|
| 靶点 |
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| 体内研究(In Vivo) | ||
| 体内研究活性 | 体内研究表明AG1343在多个物种口服后能很好地被吸收，在人类中具有良好的药代动力学特征。在饲养大鼠中，该化合物的口服生物利用度为43%，而在禁食大鼠中，口服生物利用度显著下降至29%。在多种生物体内，Nelfinavir的生物口服利用度为：犬类中47%、狨猴中17%、食蟹猴中26%。在口服后，其在血浆中半衰期较长，这可能是因为分解和吸收较慢的缘故。在人类中，Nelfinavir能很好地被吸收，尤其是随食物给药时，具有比较少、容易处理的副作用，安全性良好[1]。 | |
|---|---|---|
| 动物实验 | Animal Models | Sprague-Dawley rats |
| Dosages | 12.5-25 mg/kg (i.v); 25-50 mg/kg (oral) | |
| Administration | 静脉注射；口服 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00051844 | Completed | Human Immunodeficiency Virus |
Pfizer |
August 2002 | Phase 2 |
化学信息&溶解度
| 分子量 | 663.89 | 分子式 | C33H49N3O7S2 |
| CAS号 | 159989-65-8 | SDF | Download Nelfinavir Mesylate SDF |
| Smiles | CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O.CS(=O)(=O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (150.62 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL (150.62 mM) Water : Insoluble |
摩尔浓度计算器 |
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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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