1. Anti-infection Metabolic Enzyme/Protease
  2. HIV HIV Protease SARS-CoV
  3. Amprenavir

Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.

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Amprenavir Chemical Structure

Amprenavir Chemical Structure

CAS No. : 161814-49-9

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Customer Review

Based on 7 publication(s) in Google Scholar

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Description

Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.

IC50 & Target

IC50 Value: 0.6 nM (Ki); Against wild-type clinical HIV isolates:14.6 +/- 12.5 ng/mL (mean +/- SD) [1]. Target: HIV protease

Cellular Effect
Cell Line Type Value Description References
C8166 CC50
0.23 mM
Compound: APV
Cytostatic activity against human C8166 cells by MTT assay
Cytostatic activity against human C8166 cells by MTT assay
[PMID: 22306123]
C8166 EC50
2.93 nM
Compound: APV
Antiviral activity against HIV1 3B infected in human C8166 cells assessed as inhibition of syncytia formation after 3 days
Antiviral activity against HIV1 3B infected in human C8166 cells assessed as inhibition of syncytia formation after 3 days
[PMID: 22306123]
CCRF-CEM EC50
404 nM
Compound: APV
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
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
[PMID: 17576848]
CCRF-CEM EC50
583 nM
Compound: APV
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
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
[PMID: 17576848]
CCRF-CEM EC50
630 nM
Compound: APV
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
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
[PMID: 17576848]
CCRF-CEM EC50
855 nM
Compound: APV
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
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
[PMID: 17576848]
HEK293 EC50
1.8 nM
Compound: 1, APV
Antiviral activity against wild type HIV1 clade B isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
Antiviral activity against wild type HIV1 clade B isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
[PMID: 22708897]
HEK293 EC50
10.7 nM
Compound: APV
Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay
Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay
[PMID: 17638694]
HEK293 EC50
15.6 nM
Compound: 1, APV
Antiviral activity against multidrug resistant HIV1 MDR1 containing protease M46I, I54V, V82A and L90M mutant infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
Antiviral activity against multidrug resistant HIV1 MDR1 containing protease M46I, I54V, V82A and L90M mutant infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
[PMID: 22708897]
HEK293 EC50
17.5 nM
Compound: 1, APV
Antiviral activity against multidrug resistant HIV1 MDRC4 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
Antiviral activity against multidrug resistant HIV1 MDRC4 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
[PMID: 22708897]
HEK293 EC50
2.6 nM
Compound: 1, APV
Antiviral activity against wild type HIV1 clade A isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
Antiviral activity against wild type HIV1 clade A isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
[PMID: 22708897]
HEK293 EC50
3 nM
Compound: 1, APV
Antiviral activity against wild type HIV1 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
Antiviral activity against wild type HIV1 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
[PMID: 22708897]
HEK293 EC50
3.7 nM
Compound: 1, APV
Antiviral activity against wild type HIV1 clade C isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
Antiviral activity against wild type HIV1 clade C isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay
[PMID: 22708897]
HepG2 CC50
98.4 μM
Compound: Amprenavir
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay
10.1039/C1MD00147G
MT2 CC50
> 100 μM
Compound: APV
Cytotoxicity against human MT2 cells after 7 days by MTT assay
Cytotoxicity against human MT2 cells after 7 days by MTT assay
[PMID: 20439612]
MT2 CC50
> 100 μM
Compound: APV
Cytotoxicity against human MT2 cells by MTT assay
Cytotoxicity against human MT2 cells by MTT assay
[PMID: 18955518]
MT2 CC50
> 100 μM
Compound: amprenavir, APV
Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT2 CC50
> 100 μM
Compound: Amprenavir
Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay
Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay
10.1039/C1MD00147G
MT2 EC50
0.024 μM
Compound: APV
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
[PMID: 20439612]
MT2 IC50
0.03 μM
Compound: APV
Antiviral activity against HIV1 LAI infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
Antiviral activity against HIV1 LAI infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
[PMID: 21194227]
MT2 EC50
0.033 μM
Compound: APV
Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay
Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay
[PMID: 18955518]
MT2 EC50
0.036 μM
Compound: amprenavir, APV
Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT2 EC50
0.12 μM
Compound: APV
Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay
Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay
[PMID: 20439612]
MT2 EC50
0.25 μM
Compound: amprenavir, APV
Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT2 EC50
0.42 μM
Compound: APV
Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay
Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay
[PMID: 20439612]
MT2 EC50
0.57 μM
Compound: amprenavir, APV
Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT2 EC50
24 nM
Compound: Amprenavir
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay
10.1039/C1MD00147G
MT2 IC50
30 nM
Compound: APV
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
[PMID: 23947685]
MT4 EC50
> 1 μM
Compound: APV
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
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
[PMID: 18955518]
MT4 EC50
> 1 μM
Compound: APV
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
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
[PMID: 20439612]
MT4 EC50
> 1 μM
Compound: APV
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
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
[PMID: 20439612]
MT4 EC50
> 1 μM
Compound: amprenavir, APV
Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 EC50
> 1 μM
Compound: amprenavir, APV
Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 CC50
> 100 μM
Compound: APV
Cytotoxicity against human MT4 cells after 6 days by MTT assay
Cytotoxicity against human MT4 cells after 6 days by MTT assay
[PMID: 17638694]
MT4 CC50
> 100 μM
Compound: APV
Cytotoxicity against human MT4 cells by MTT assay
Cytotoxicity against human MT4 cells by MTT assay
[PMID: 17548498]
MT4 EC50
0.01 μM
Compound: Amprenavir
Concentration required to inhibit syncytia formation by 50% on MT-4 cells.
Concentration required to inhibit syncytia formation by 50% on MT-4 cells.
[PMID: 12109915]
MT4 EC50
0.024 μM
Compound: APV
Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay
Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay
[PMID: 17548498]
MT4 EC50
0.026 μM
Compound: amprenavir, APV
Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay
Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay
[PMID: 17371811]
MT4 EC50
0.028 μM
Compound: APV
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA
[PMID: 18955518]
MT4 EC50
0.028 μM
Compound: APV
Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay
Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay
[PMID: 20439612]
MT4 EC50
0.034 μM
Compound: APV
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay
[PMID: 20439612]
MT4 EC50
0.037 μM
Compound: APV
Antiviral activity against wild type HIV1 ERS104P infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay
Antiviral activity against wild type HIV1 ERS104P infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay
[PMID: 26107245]
MT4 EC50
0.04 μM
Compound: APV, amprenavir
Antiviral activity against HIV1 infected MT4 cells by MTT method
Antiviral activity against HIV1 infected MT4 cells by MTT method
[PMID: 17696512]
MT4 EC50
0.051 μM
Compound: APV
Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay
Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay
[PMID: 17638694]
MT4 EC50
0.058 μM
Compound: amprenavir, APV
Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 EC50
0.06 μM
Compound: amprenavir, APV
Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 EC50
0.078 μM
Compound: APV
Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S 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 nelfinavir by ELISA
Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S 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 nelfinavir by ELISA
[PMID: 18955518]
MT4 EC50
0.17 μM
Compound: amprenavir, APV
Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 EC50
0.18 μM
Compound: APV
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
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
[PMID: 18955518]
MT4 EC50
0.18 μM
Compound: APV
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
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
[PMID: 20439612]
MT4 EC50
0.2 μM
Compound: amprenavir, APV
Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 EC50
0.21 μM
Compound: APV
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
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
[PMID: 18955518]
MT4 EC50
0.21 μM
Compound: APV
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
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
[PMID: 18955518]
MT4 EC50
0.26 μM
Compound: APV
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
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
[PMID: 18955518]
MT4 EC50
0.26 μM
Compound: APV
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
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
[PMID: 20439612]
MT4 EC50
0.26 μM
Compound: APV
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
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
[PMID: 20439612]
MT4 EC50
0.28 μM
Compound: APV
Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay
Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay
[PMID: 20439612]
MT4 EC50
0.28 μM
Compound: amprenavir, APV
Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 EC50
0.31 μM
Compound: amprenavir, APV
Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 EC50
0.32 μM
Compound: APV
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
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
[PMID: 18955518]
MT4 EC50
0.33 μM
Compound: amprenavir, APV
Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 EC50
0.33 μM
Compound: amprenavir, APV
Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
[PMID: 17371811]
MT4 EC50
0.34 μM
Compound: APV
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
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
[PMID: 20439612]
MT4 EC50
0.35 μM
Compound: APV
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
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
[PMID: 20439612]
MT4 EC50
0.43 μM
Compound: APV
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
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
[PMID: 18955518]
MT4 EC50
72 nM
Compound: APV
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
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
[PMID: 17576848]
MT4 EC50
900 nM
Compound: APV
Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
[PMID: 17576848]
PBMC EC50
> 1 μM
Compound: APV
Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
[PMID: 20439612]
PBMC CC50
> 100 μM
Compound: APV
Cytotoxicity against human PHA-PBMC cells by MTT assay
Cytotoxicity against human PHA-PBMC cells by MTT assay
[PMID: 17548498]
PBMC EC50
> 1000 nM
Compound: 5; APV
Antiviral activity against darunavir-resistant HIV1 10P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
Antiviral activity against darunavir-resistant HIV1 10P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
[PMID: 26799988]
PBMC EC50
> 1000 nM
Compound: 5; APV
Antiviral activity against darunavir-resistant HIV1 20P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
Antiviral activity against darunavir-resistant HIV1 20P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
[PMID: 26799988]
PBMC EC50
0.029 μM
Compound: 5; APV
Antiviral activity against wild type HIV1 ERS104pre infected in human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
Antiviral activity against wild type HIV1 ERS104pre infected in human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
[PMID: 26799988]
PBMC EC50
0.03 μM
Compound: APV
Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay
[PMID: 20439612]
PBMC EC50
0.21 μM
Compound: 5; APV
Antiviral activity against multidrug-resistant HIV1-C infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
Antiviral activity against multidrug-resistant HIV1-C infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
[PMID: 26799988]
PBMC EC50
0.21 μM
Compound: APV
Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay
[PMID: 20439612]
PBMC EC50
0.27 μM
Compound: 5; APV
Antiviral activity against multidrug-resistant HIV1-MM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
Antiviral activity against multidrug-resistant HIV1-MM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
[PMID: 26799988]
PBMC EC50
0.3 μM
Compound: 5; APV
Antiviral activity against multidrug-resistant HIV1-TM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
Antiviral activity against multidrug-resistant HIV1-TM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
[PMID: 26799988]
PBMC EC50
0.31 μM
Compound: 5; APV
Antiviral activity against multidrug-resistant HIV1-G infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
Antiviral activity against multidrug-resistant HIV1-G infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
[PMID: 26799988]
PBMC EC50
0.32 μM
Compound: APV
Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
[PMID: 20439612]
PBMC EC50
0.36 μM
Compound: 5; APV
Antiviral activity against multidrug-resistant HIV1-B infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
Antiviral activity against multidrug-resistant HIV1-B infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
[PMID: 26799988]
PBMC EC50
0.37 μM
Compound: APV
Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay
[PMID: 20439612]
PBMC EC50
0.43 μM
Compound: 5; APV
Antiviral activity against multidrug-resistant HIV1-JSL infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
Antiviral activity against multidrug-resistant HIV1-JSL infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay
[PMID: 26799988]
PBMC EC50
0.43 μM
Compound: APV
Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay
[PMID: 20439612]
PBMC EC50
0.62 μM
Compound: APV
Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay
[PMID: 20439612]
SUP-T1 EC50
> 1000 nM
Compound: APV
Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of integrated junction products after 48 hrs by Alu-PCR assay
Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of integrated junction products after 48 hrs by Alu-PCR assay
[PMID: 19104010]
SUP-T1 EC50
> 1000 nM
Compound: APV
Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of late RT products after 12 hrs
Antiviral activity against HIV1 infected in SupT1 cells assessed as accumulation of late RT products after 12 hrs
[PMID: 19104010]
In Vitro

Amprenavir has an enzyme inhibition constant (Ki = 0.6 nM) that falls within the Ki range of the other protease inhibitors. Amprenavir's in vitro 50% inhibitory concentration (IC50) against wild-type clinical HIV isolates is 14.6 +/- 12.5 ng/mL (mean +/- SD) [1]. Amprenavir had direct inhibitory effects on invasion of Huh-7 hepatocarcinoma cell lines, inhibiting MMP proteolytic activation [2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Amprenavir was able to promote regression of hepatocarcinoma growth in vivo by anti-angiogenetic and overall anti-tumor activities, independently by PI3K/AKT related pathways that at today is one of the more suggestive hypothesis to explain the anti-tumor effects of the different protease inhibitors [2]. Amprenavir efficiently activated PXR and induced PXR target gene expression in vitro and in vivo. Short-term exposure to amprenavirsignificantly increased plasma total cholesterol and atherogenic low-density lipoprotein cholesterol levels in wild-type mice, but not in PXR-deficient mice [3]. Amprenavir has been approved for adults and children; the recommended capsule doses are 1200 mg twice daily for adults and 20 mg/kg twice daily or 15 mg/kg 3 times daily for children < 13 years of age or adolescents < 50 kg [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

505.63

Formula

C25H35N3O6S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[C@@H]1COCC1)N[C@@H](CC2=CC=CC=C2)[C@H](O)CN(S(=O)(C3=CC=C(N)C=C3)=O)CC(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (197.77 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9777 mL 9.8887 mL 19.7773 mL
5 mM 0.3955 mL 1.9777 mL 3.9555 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.53%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9777 mL 9.8887 mL 19.7773 mL 49.4433 mL
5 mM 0.3955 mL 1.9777 mL 3.9555 mL 9.8887 mL
10 mM 0.1978 mL 0.9889 mL 1.9777 mL 4.9443 mL
15 mM 0.1318 mL 0.6592 mL 1.3185 mL 3.2962 mL
20 mM 0.0989 mL 0.4944 mL 0.9889 mL 2.4722 mL
25 mM 0.0791 mL 0.3955 mL 0.7911 mL 1.9777 mL
30 mM 0.0659 mL 0.3296 mL 0.6592 mL 1.6481 mL
40 mM 0.0494 mL 0.2472 mL 0.4944 mL 1.2361 mL
50 mM 0.0396 mL 0.1978 mL 0.3955 mL 0.9889 mL
60 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8241 mL
80 mM 0.0247 mL 0.1236 mL 0.2472 mL 0.6180 mL
100 mM 0.0198 mL 0.0989 mL 0.1978 mL 0.4944 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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