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Nelfinavir Mesylate

別名: AG 1343 Mesylate 中文名稱：甲磺酸奈非那韋

Nelfinavir Mesylate是強(qiáng)效的HIV protease抑制劑，Ki為2 nM。

Nelfinavir Mesylate Chemical Structure

Nelfinavir Mesylate Chemical Structure

CAS: 159989-65-8

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 1203.93 現(xiàn)貨
10mg 1117.15 現(xiàn)貨
50mg 3349.71 現(xiàn)貨
200mg 8165.43 現(xiàn)貨
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Nelfinavir Mesylate相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

HIV Protease Signaling Pathways

HIV Protease信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Nelfinavir Mesylate是強(qiáng)效的HIV protease抑制劑，Ki為2 nM。
靶點(diǎn)
HIV protease [1]
(Cell-free assay)
2 nM(Ki)
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 體內(nèi)研究表明AG1343在多個(gè)物種口服后能很好地被吸收，在人類中具有良好的藥代動(dòng)力學(xué)特征。在飼養(yǎng)大鼠中，該化合物的口服生物利用度為43%，而在禁食大鼠中，口服生物利用度顯著下降至29%。在多種生物體內(nèi)，Nelfinavir的生物口服利用度為：犬類中47%、狨猴中17%、食蟹猴中26%。在口服后，其在血漿中半衰期較長(zhǎng)，這可能是因?yàn)榉纸夂臀蛰^慢的緣故。在人類中，Nelfinavir能很好地被吸收，尤其是隨食物給藥時(shí)，具有比較少、容易處理的副作用，安全性良好[1]。
動(dòng)物實(shí)驗(yàn) Animal Models Sprague-Dawley rats
Dosages 12.5-25 mg/kg (i.v); 25-50 mg/kg (oral)
Administration 靜脈注射；口服
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00051844 Completed
Human Immunodeficiency Virus
Pfizer
 August 2002 Phase 2

化學(xué)信息&溶解度

分子量 663.89 分子式

C33H49N3O7S2
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (150.62 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 100 mg/mL (150.62 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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