Art. -Nr.: HY-17430

Amprenavir

(Synonyms: VX-478)

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

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Reinheit: 99.55%
CAS. Nr.: 161814-49-9
Formel: C₂₅H₃₅N₃O₆S
Molecular Weight:505.63

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Amprenavir Chemical Structure

CAS. Nr.: 161814-49-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
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- In Vitro
- In Vivo
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Biologische Aktivität

Beschreibung

Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CL^pro 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

Alle HIV Isoform-spezifische Produkte anzeigen :

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	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	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	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]
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]
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	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	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	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	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	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	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	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]
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	0.036 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	0.25 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	0.57 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	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	CC₅₀	>100 μM Compound: APV	Cytotoxicity against human MT2 cells by MTT assay Cytotoxicity against human MT2 cells by MTT assay	[PMID: 18955518]
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	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	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	0.12 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	0.42 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	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	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	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	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
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	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	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	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	>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	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	0.15 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	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: 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	>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	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	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	>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	130 nM Compound: amprenavir	Antiviral activity against HIV1 HXB2 in MT4 cells Antiviral activity against HIV1 HXB2 in MT4 cells	[PMID: 16458505]
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 HIV D545701 in MT4 cells Antiviral activity against HIV D545701 in MT4 cells	[PMID: 16458505]
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	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	0.058 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	0.17 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	0.2 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	0.28 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	0.33 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	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	0.024 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	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	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	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	0.04 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	>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	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	0.078 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	0.18 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	0.21 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	0.21 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	0.32 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	0.43 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	>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	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	0.18 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	0.26 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	0.34 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	0.037 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	0.044 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	0.38 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]
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]
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	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	>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	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: 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	0.32 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	0.37 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: 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]
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	0.325 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	0.426 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	0.448 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	>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	0.21 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	0.27 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	0.36 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	0.43 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	>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]
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]
SUP-T1	CC₅₀	96 μM 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]

In Vitro

Amprenavir has an enzyme inhibition constant (K_i = 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.

In Vivo

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 161814-49-9
Appearance Solid
Molecular Weight 505.63
Formel C₂₅H₃₅N₃O₆S
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
Synonyms

VX-478
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

All

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Journal Impact Factor

Signal Transduct Target Ther

Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. [Abstract]

2021 May 29;6(1):212. PMID: 34052830
Nat Commun

Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. [Abstract]

2020 Sep 4;11(1):4417. PMID: 32887884
J Med Chem

Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]

2021 Mar 11;64(5):2725-2738. PMID: 33619967
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
Antimicrob Agents Chemother

Discovery of M Protease Inhibitors Encoded by SARS-CoV-2. [Abstract]

2020 Aug 20;64(9):e00872-20. PMID: 32669265
Laryngoscope Investig Otolaryngol

Inhaled fosamprenavir for laryngopharyngeal reflux: Toxicology and fluid dynamics modeling. [Abstract]

2024 Jan 24;9(1):e1219. PMID: 38362183
bioRxiv

2020 Apr.

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sadler BM, Stein DS. Clinical pharmacology and pharmacokinetics of amprenavir. Ann Pharmacother. 2002 Jan;36(1):102-18. [Content Brief]

[2]. Esposito V, Verdina A, Manente L, Amprenavir inhibits the migration in human hepatocarcinoma cell and the growth of xenografts. J Cell Physiol. 2013 Mar;228(3):640-5. [Content Brief]

[3]. Helsley RN, Sui Y, Ai N, Pregnane X Receptor Mediates Dyslipidemia Induced by the HIV Protease Inhibitor Amprenavir in Mice. Mol Pharmacol. 2013 Jun;83(6):1190-9. [Content Brief]

[4]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Amprenavir

7 Cited Publications

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Amprenavir

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

CNS-Penetrant Compound Library

Peptidomimetic Library

Drug Repurposing Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

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Publications Citing Use of MedChemExpress (MCE) Amprenavir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Amprenavir

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

CNS-Penetrant Compound Library

Peptidomimetic Library

Drug Repurposing Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Protease Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Publications Citing Use of MedChemExpress (MCE) Amprenavir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Amprenavir Related Classifications

HY-17430 Related Classifications