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

Amprenavir 構造式

CAS 番号 : 161814-49-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 在庫あり
Solution
10 mM * 1 mL in DMSO USD 73 在庫あり
Solid
5 mg $66 在庫あり
25 mg $160 在庫あり
50 mg $260 在庫あり
100 mg $416 在庫あり
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カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of Amprenavir:

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製品説明

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]
HEK-293T CC50
> 200 μM
Compound: 3; APV
Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37120996]
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
MDCK-II IC50
> 100 μM
Compound: APV
Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells
Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells
[PMID: 17664327]
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: 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: 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 CC50
> 100 μM
Compound: Amprenavir
Anti-HIV activity based on reduction of the viability of mock-infected MT-2 cells.
Anti-HIV activity based on reduction of the viability of mock-infected MT-2 cells.
[PMID: 12699395]
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 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 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
0.028 μM
Compound: Amprenavir
Compound tested for the inhibition of HIV-induced cytopathogenicity in MT-2 cells
Compound tested for the inhibition of HIV-induced cytopathogenicity in MT-2 cells
[PMID: 15887965]
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 IC50
0.03 μM
Compound: APV
Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT2 cells assessed as inhibition of p24 Gag protein production
Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT2 cells assessed as inhibition of p24 Gag protein production
[PMID: 21800876]
MT2 IC50
0.03 μM
Compound: amprenavir VX-478
Inhibition of virion associated RT activity relative to untreated, infected control in MT2 cells infected with HIV-1 237288 strain
Inhibition of virion associated RT activity relative to untreated, infected control in MT2 cells infected with HIV-1 237288 strain
[PMID: 11000004]
MT2 IC50
24 nM
Compound: APV
Antiviral activity against HIV1 LAI isolate in human MT2 cells
Antiviral activity against HIV1 LAI isolate in human MT2 cells
[PMID: 16913714]
MT2 IC50
27 nM
Compound: APV
Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of virus-induced cytopathic effect
Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of virus-induced cytopathic effect
[PMID: 18783203]
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]
MT2 IC50
30 nM
Compound: Amprenavir
Concentration required to produce 50% reduction in virion associated RT activity in HIV-1 infected MT2 cells
Concentration required to produce 50% reduction in virion associated RT activity in HIV-1 infected MT2 cells
[PMID: 11784141]
MT2 IC50
36 nM
Compound: Amprenavir
Anti-HIV activity based on inhibition of HIV-1 induced cytopathogenicity in MT-2 cells.
Anti-HIV activity based on inhibition of HIV-1 induced cytopathogenicity in MT-2 cells.
[PMID: 12699395]
MT2 IC50
440 nM
Compound: APV
Antiviral activity against HIV2 EHO isolate in human MT2 cells
Antiviral activity against HIV2 EHO isolate in human MT2 cells
[PMID: 16913714]
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 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
> 50 μM
Compound: Amprenavir
Concentration required to cause 50% death of uninfected MT-4 cells.
Concentration required to cause 50% death of uninfected MT-4 cells.
[PMID: 12109915]
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
0.044 μM
Compound: APV
Antiviral activity against multidrug resistant HIV1 MDR/B containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production
Antiviral activity against multidrug resistant HIV1 MDR/B containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production
[PMID: 26107245]
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 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 ELISA
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 ELISA
[PMID: 18955518]
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
0.26 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 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
0.33 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
0.34 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
0.38 μM
Compound: APV
Antiviral activity against multidrug resistant HIV1 MDR/C containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production
Antiviral activity against multidrug resistant HIV1 MDR/C containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production
[PMID: 26107245]
MT4 EC50
0.398 μM
Compound: APV
Antiviral activity against multidrug resistant HIV1 MDR/G containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production
Antiviral activity against multidrug resistant HIV1 MDR/G containing protease mutant infected in human MT4 cells assessed as inhibition of p24 Gag protein production
[PMID: 26107245]
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]
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 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 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 ED50
0.08 μM
Compound: Amprenavir
Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells
Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells
[PMID: 15537350]
MT4 IC50
0.1 μM
Compound: Amprenavir
Compound was evaluated for its antiviral inhibition in MT-4 cell culture
Compound was evaluated for its antiviral inhibition in MT-4 cell culture
[PMID: 10866371]
MT4 IC50
0.15 μM
Compound: Amprenavir
Antiviral inhibitory concentration against human immunodeficiency virus type 1 in MT-4 cell culture
Antiviral inhibitory concentration against human immunodeficiency virus type 1 in MT-4 cell culture
[PMID: 15582415]
MT4 IC50
130 nM
Compound: Amprenavir
Antiviral activity against wild-type HIV virus (HXB2) was determined in MT-4 cell line
Antiviral activity against wild-type HIV virus (HXB2) was determined in MT-4 cell line
[PMID: 15013001]
MT4 IC50
130 nM
Compound: Amprenavir
Inhibitory concentration against wild type Human immuno deficiency virus (HXB2) was determined in an MT-4 cell line
Inhibitory concentration against wild type Human immuno deficiency virus (HXB2) was determined in an MT-4 cell line
[PMID: 15990305]
MT4 IC50
130 nM
Compound: amprenavir
Antiviral activity against HIV1 HXB2 in MT4 cells
Antiviral activity against HIV1 HXB2 in MT4 cells
[PMID: 16458505]
MT4 IC50
150 nM
Compound: Entry Amprenavir
Inhibitory concentration for antiviral inhibition against HIV-1 in MT-4 cell culture
Inhibitory concentration for antiviral inhibition against HIV-1 in MT-4 cell culture
[PMID: 15975788]
MT4 IC50
440 nM
Compound: Amprenavir
Antiviral activity against PI resistant virus EP13 was determined in MT-4 cell line
Antiviral activity against PI resistant virus EP13 was determined in MT-4 cell line
[PMID: 15013001]
MT4 IC50
440 nM
Compound: Amprenavir
Inhibitory concentration against wild type Human immuno deficiency virus (EP13) was determined in an MT-4 cell line
Inhibitory concentration against wild type Human immuno deficiency virus (EP13) was determined in an MT-4 cell line
[PMID: 15990305]
MT4 IC50
440 nM
Compound: Entry Amprenavir
Inhibitory concentration against multi-PI resistant EP13 in MT-4 cell lines(fold range = 3)
Inhibitory concentration against multi-PI resistant EP13 in MT-4 cell lines(fold range = 3)
[PMID: 15975788]
MT4 IC50
440 nM
Compound: amprenavir
Antiviral activity against HIV1 EP13 in MT4 cells
Antiviral activity against HIV1 EP13 in MT4 cells
[PMID: 16458505]
MT4 IC50
> 1000 nM
Compound: Amprenavir
Antiviral activity against PI resistant virus D545701 was determined in MT-4 cell line
Antiviral activity against PI resistant virus D545701 was determined in MT-4 cell line
[PMID: 15013001]
MT4 IC50
> 1000 nM
Compound: Amprenavir
Inhibitory concentration against wild type Human immuno deficiency virus (D545701) was determined in an MT-4 cell line
Inhibitory concentration against wild type Human immuno deficiency virus (D545701) was determined in an MT-4 cell line
[PMID: 15990305]
MT4 IC50
> 1000 nM
Compound: Entry Amprenavir
Inhibitory concentration against multi-PI resistant D545701 in MT-4 cell lines(fold range > 7)
Inhibitory concentration against multi-PI resistant D545701 in MT-4 cell lines(fold range > 7)
[PMID: 15975788]
MT4 IC50
> 1000 nM
Compound: amprenavir
Antiviral activity against HIV D545701 in MT4 cells
Antiviral activity against HIV D545701 in MT4 cells
[PMID: 16458505]
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
0.028 μM
Compound: APV
Antiviral activity against wild type HIV1 ERS104pre infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production
Antiviral activity against wild type HIV1 ERS104pre infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production
[PMID: 23947685]
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
0.325 μM
Compound: APV
Antiviral activity against multidrug-resistant HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production
Antiviral activity against multidrug-resistant HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production
[PMID: 23947685]
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
0.426 μM
Compound: APV
Antiviral activity against multidrug-resistant HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production.
Antiviral activity against multidrug-resistant HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production.
[PMID: 23947685]
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
0.448 μM
Compound: APV
Antiviral activity against multidrug-resistant HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production
Antiviral activity against multidrug-resistant HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L protease-encoding region mutant infected in human PHA-PBMC cells assessed as inhibition of p24 Gag protein production
[PMID: 23947685]
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]
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 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 IC50
220 nM
Compound: APV
Antiviral activity against multi drug-resistant HIV1 TM variant in human PHA-PBMC cells
Antiviral activity against multi drug-resistant HIV1 TM variant in human PHA-PBMC cells
[PMID: 16913714]
PBMC IC50
23 nM
Compound: APV
Antiviral activity against multi drug-resistant HIV1 ET variant in human PHA-PBMC cells
Antiviral activity against multi drug-resistant HIV1 ET variant in human PHA-PBMC cells
[PMID: 16913714]
PBMC IC50
29 nM
Compound: APV
Antiviral activity against HIV1 BA-L isolate in human PHA-PBMC cells
Antiviral activity against HIV1 BA-L isolate in human PHA-PBMC cells
[PMID: 16913714]
PBMC IC50
290 nM
Compound: APV
Antiviral activity against multi drug-resistant HIV1 B variant in human PHA-PBMC cells
Antiviral activity against multi drug-resistant HIV1 B variant in human PHA-PBMC cells
[PMID: 16913714]
PBMC IC50
300 nM
Compound: APV
Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells
Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells
[PMID: 16913714]
PBMC IC50
310 nM
Compound: APV
Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells
Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells
[PMID: 16913714]
PBMC IC50
34 nM
Compound: APV
Antiviral activity against HIV1 LAI isolate in human PHA-PBMC cells
Antiviral activity against HIV1 LAI isolate in human PHA-PBMC cells
[PMID: 16913714]
PBMC IC50
68 nM
Compound: APV
Antiviral activity against multi drug-resistant HIV1 K variant in human PHA-PBMC cells
Antiviral activity against multi drug-resistant HIV1 K variant in human PHA-PBMC cells
[PMID: 16913714]
PBMC IC50
> 1000 nM
Compound: APV
Antiviral activity against multi drug-resistant HIV1 ES variant in human PHA-PBMC cells
Antiviral activity against multi drug-resistant HIV1 ES variant in human PHA-PBMC cells
[PMID: 16913714]
PBMC IC50
> 1000 nM
Compound: APV
Antiviral activity against multi drug-resistant HIV1 EV variant in human PHA-PBMC cells
Antiviral activity against multi drug-resistant HIV1 EV variant in human PHA-PBMC cells
[PMID: 16913714]
SUP-T1 CC50
96000 nM
Compound: APV
Cytotoxicity against human SupT1 cells infected with HIV1 3B
Cytotoxicity against human SupT1 cells infected with HIV1 3B
[PMID: 19104010]
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]
体外実験

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 ng/mL[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.

体内実験

Amprenavir is 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 activates PXR and induces PXR target gene expression in vitro and in vivo. Short-term exposure to amprenavirsignificantly increases plasma total cholesterol and atherogenic low-density lipoprotein cholesterol levels in wild-type mice, but not in PXR-deficient mice[3].

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

臨床実験
分子量

505.63

分子式

C25H35N3O6S

CAS 番号
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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.1978 mL 0.9889 mL 1.9777 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)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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.
純度とドキュメンテーション

純度: 99.55%

参考文献

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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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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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製品名:
Amprenavir
製品番号:
HY-17430
数量:
MCE 日本正規代理店: