1. Anti-infection Metabolic Enzyme/Protease
  2. HIV HIV Protease
  3. Darunavir

Darunavir  (Synonyms: TMC114; UIC-94017)

Cat. No.: HY-17040 Purity: 99.91%
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Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity.

For research use only. We do not sell to patients.

Darunavir Chemical Structure

Darunavir Chemical Structure

CAS No. : 206361-99-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 48 In-stock
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Customer Review

Based on 11 publication(s) in Google Scholar

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Description

Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity[1][2].

IC50 & Target

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
CCRF-CEM EC50
10 nM
Compound: DRV
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
6 nM
Compound: DRV
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
8 nM
Compound: DRV
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
9 nM
Compound: DRV
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
0.15 nM
Compound: 2, DRV
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
0.18 nM
Compound: 2, DRV
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]
HEK293 EC50
0.23 nM
Compound: 2, DRV
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
0.25 nM
Compound: 2, DRV
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
0.3 nM
Compound: 2, DRV
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
0.6 nM
Compound: 2, DRV
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]
HEK-293T CC50
> 100 μM
Compound: DRV
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
[PMID: 35483138]
HEK-293T CC50
> 100 μM
Compound: DRV
Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay
[PMID: 33906049]
HEK-293T CC50
> 100 μM
Compound: DRV
Cytotoxicity against human 293T cells measured after 24 hrs by CCK8 assay
Cytotoxicity against human 293T cells measured after 24 hrs by CCK8 assay
[PMID: 31734023]
HEK-293T CC50
> 200 μM
Compound: DRV
Cytotoxicity against human HEK-293T cells after 24 hrs by CCK-8 assay
Cytotoxicity against human HEK-293T cells after 24 hrs by CCK-8 assay
[PMID: 35278855]
HEK-293T EC50
13660 nM
Compound: darunavir
Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay
Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay
[PMID: 22148316]
HepG2 CC50
95.5 μM
Compound: 2, TMC-114
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay
10.1039/C1MD00147G
MT2 CC50
> 100 μM
Compound: DRV
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: 2, TMC-114
Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay
Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay
10.1039/C1MD00147G
MT2 EC50
0.003 μM
Compound: DRV
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
0.0039 μM
Compound: darunavir, DRV
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
0.0068 μM
Compound: darunavir, DRV
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
0.008 μM
Compound: DRV
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
0.008 μM
Compound: darunavir, DRV
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
0.01 μM
Compound: DRV
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
1.6 nM
Compound: 1, DRV
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: 19746963]
MT2 EC50
2.3 nM
Compound: 2, TMC-114
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
3 nM
Compound: Darunavir
Antiviral activity against HIV-1 LAI infected in MT-2 cells measured after 7 days by MTT assay
Antiviral activity against HIV-1 LAI infected in MT-2 cells measured after 7 days by MTT assay
[PMID: 26096678]
MT2 IC50
3 nM
Compound: 2, DRV
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
83.1 μM
Compound: darunavir, DRV
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]
MT4 EC50
> 100 nM
Compound: DPV
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay
[PMID: 18212102]
MT4 EC50
0.0026 μM
Compound: DRV
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells by XTT assay
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells by XTT assay
[PMID: 26306007]
MT4 EC50
0.003 μM
Compound: DRV
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
0.003 μM
Compound: DRV
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
0.003 μM
Compound: darunavir, DRV
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
0.0033 μM
Compound: darunavir, DRV
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
0.0034 μM
Compound: darunavir, DRV
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
0.0035 μM
Compound: DRV
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
0.0058 μM
Compound: darunavir, DRV
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
0.006 μM
Compound: DRV
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
0.009 μM
Compound: DRV
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
0.009 μM
Compound: DRV
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
0.015 μM
Compound: darunavir, DRV
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
0.016 μM
Compound: DRV
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
0.018 μM
Compound: darunavir, DRV
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
0.021 μM
Compound: darunavir, DRV
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
0.025 μM
Compound: DRV
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
0.029 μM
Compound: DRV
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
0.031 μM
Compound: DRV
Antiviral activity against darunavir-resistant HIV1 P10 infected in human MT4 cells by XTT assay
Antiviral activity against darunavir-resistant HIV1 P10 infected in human MT4 cells by XTT assay
[PMID: 26306007]
MT4 EC50
0.036 μM
Compound: darunavir, DRV
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
0.097 μM
Compound: DRV
Antiviral activity against darunavir-resistant HIV1 P20 infected in human MT4 cells by XTT assay
Antiviral activity against darunavir-resistant HIV1 P20 infected in human MT4 cells by XTT assay
[PMID: 26306007]
MT4 EC50
0.2 μM
Compound: DRV
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
0.21 μM
Compound: darunavir, DRV
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
0.29 μM
Compound: DRV
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
0.33 μM
Compound: darunavir, DRV
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 IC50
10 nM
Compound: DRV
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M6 mutant infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M6 mutant infected in human MT4 cells after 5 days by MTT assay
[PMID: 22749283]
MT4 EC50
11 nM
Compound: DRV
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 40% fetal bovine serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 40% fetal bovine serum by MTS assay
[PMID: 17620375]
MT4 EC50
11 nM
Compound: DRV
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay
[PMID: 17620375]
MT4 IC50
11 nM
Compound: DRV
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M3 mutant infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M3 mutant infected in human MT4 cells after 5 days by MTT assay
[PMID: 22749283]
MT4 EC50
12 nM
Compound: DRV
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay
[PMID: 19323562]
MT4 EC50
12 nM
Compound: DRV
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
12 nM
Compound: DPV
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay
[PMID: 18212102]
MT4 IC50
130 nM
Compound: DRV
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M10 mutant infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M10 mutant infected in human MT4 cells after 5 days by MTT assay
[PMID: 22749283]
MT4 EC50
15 nM
Compound: DRV
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay
[PMID: 17620375]
MT4 IC50
16 nM
Compound: DRV
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M8 mutant infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M8 mutant infected in human MT4 cells after 5 days by MTT assay
[PMID: 22749283]
MT4 EC50
19 nM
Compound: DRV
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay
[PMID: 17620375]
MT4 EC50
22 nM
Compound: DRV
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay
[PMID: 17620375]
MT4 IC50
22 nM
Compound: DRV
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M5 mutant infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M5 mutant infected in human MT4 cells after 5 days by MTT assay
[PMID: 22749283]
MT4 IC50
25 nM
Compound: DRV
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M9 mutant infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M9 mutant infected in human MT4 cells after 5 days by MTT assay
[PMID: 22749283]
MT4 IC50
3 nM
Compound: DRV
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing wild type protease infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing wild type protease infected in human MT4 cells after 5 days by MTT assay
[PMID: 22749283]
MT4 IC50
3.2 nM
Compound: DRV
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M7 mutant infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M7 mutant infected in human MT4 cells after 5 days by MTT assay
[PMID: 22749283]
MT4 EC50
3.5 μM
Compound: DRV
Antiviral activity against darunavir-resistant HIV1 P51 infected in human MT4 cells by XTT assay
Antiviral activity against darunavir-resistant HIV1 P51 infected in human MT4 cells by XTT assay
[PMID: 26306007]
MT4 IC50
30 nM
Compound: DRV
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M4 mutant infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M4 mutant infected in human MT4 cells after 5 days by MTT assay
[PMID: 22749283]
MT4 EC50
338 nM
Compound: DRV
Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay
[PMID: 19323562]
MT4 EC50
338 nM
Compound: DPV
Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas
Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas
[PMID: 18212102]
MT4 EC50
4 nM
Compound: DRV
Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay
Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay
[PMID: 19961222]
MT4 EC50
40 nM
Compound: DPV
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay
Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay
[PMID: 18212102]
MT4 EC50
5.6 nM
Compound: DRV
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay
[PMID: 17620375]
MT4 EC50
515 nM
Compound: DRV
Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay
[PMID: 19323562]
MT4 EC50
587 nM
Compound: DRV
Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay
Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay
[PMID: 19323562]
MT4 EC50
587 nM
Compound: DPV
Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infectio
Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infectio
[PMID: 18212102]
MT4 EC50
857 nM
Compound: DPV
Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post in
Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post in
[PMID: 18212102]
PBMC EC50
> 0.025 μM
Compound: 9; DRV
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
0.003 μM
Compound: DRV
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
0.0038 μM
Compound: 9; DRV
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
0.004 μM
Compound: DRV
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
0.0043 μM
Compound: 9; DRV
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
0.005 μM
Compound: 9; DRV
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
0.007 μM
Compound: 9; DRV
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
0.008 μM
Compound: DRV
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
0.01 μM
Compound: 9; DRV
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
0.011 μM
Compound: DRV
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
0.019 μM
Compound: DRV
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
0.021 μM
Compound: 9; DRV
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
0.023 μM
Compound: DRV
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
0.027 μM
Compound: DRV
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
255.2 nM
Compound: 9; DRV
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
43.4 nM
Compound: 9; DRV
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
0.0025 μM
Compound: DRV
Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by
Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by
[PMID: 35483138]
Vero C1008 EC50
> 40 μM
Compound: Darunavir
Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days
Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days
10.1101/2020.04.03.023846
In Vitro

Darunavir (TMC114, 1a) has a stability comparable to other protease inhibitors[1].
Darunavir (TMC114, UIC-94017) blocks the infectivity and replication of each of HIV-1NL4-3 variants exposed to and selected for resistance to Ro 31-8959, MK-639, AG1341, or ABT 538 at concentrations up to 5 μM (IC50s, 0.003 to 0.029 μM), although it was less active against HIV-1NL4-3 variants selected for resistance to VX-478 (IC50, 0.22 μM)[2].

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

Clinical Trial
Molecular Weight

547.66

Formula

C27H37N3O7S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[C@@H]1[C@@]2([H])[C@@](OCC2)([H])OC1)N[C@@H](CC3=CC=CC=C3)[C@H](O)CN(S(=O)(C4=CC=C(N)C=C4)=O)CC(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : ≥ 100 mg/mL (182.60 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 1.8260 mL 9.1298 mL 18.2595 mL
5 mM 0.3652 mL 1.8260 mL 3.6519 mL
View the Complete Stock Solution Preparation Table

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

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (4.56 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 (4.56 mM); Clear solution

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

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

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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

Purity: 99.91%

References

Complete Stock Solution Preparation Table

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

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8260 mL 9.1298 mL 18.2595 mL 45.6488 mL
5 mM 0.3652 mL 1.8260 mL 3.6519 mL 9.1298 mL
10 mM 0.1826 mL 0.9130 mL 1.8260 mL 4.5649 mL
15 mM 0.1217 mL 0.6087 mL 1.2173 mL 3.0433 mL
20 mM 0.0913 mL 0.4565 mL 0.9130 mL 2.2824 mL
25 mM 0.0730 mL 0.3652 mL 0.7304 mL 1.8260 mL
30 mM 0.0609 mL 0.3043 mL 0.6087 mL 1.5216 mL
40 mM 0.0456 mL 0.2282 mL 0.4565 mL 1.1412 mL
50 mM 0.0365 mL 0.1826 mL 0.3652 mL 0.9130 mL
60 mM 0.0304 mL 0.1522 mL 0.3043 mL 0.7608 mL
80 mM 0.0228 mL 0.1141 mL 0.2282 mL 0.5706 mL
100 mM 0.0183 mL 0.0913 mL 0.1826 mL 0.4565 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

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

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