Cat. No.: HY-14588

Lopinavir

(Synonyms: ABT-378)

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Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity. Lopinavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 14.2 μM.

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Pureté: 99.71%
CAS No.: 192725-17-0
Formule: C₃₇H₄₈N₄O₅
Masse moléculaire:628.80

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Lopinavir Chemical Structure

CAS No.: 192725-17-0

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Description

Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity^[1]^[2]. Lopinavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 14.2 μM^[3].

IC₅₀ & Target

HIV-1

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Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	1.7 μM Compound: Lopinavir	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells	[PMID: 12700464]
Caco-2	CC₅₀	2128.78 μM Compound: LOPINAVIR	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	19.11 μM Compound: LOPINAVIR	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
CCRF-CEM	EC₅₀	260 nM Compound: LPV	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	28 nM Compound: LPV	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	340 nM Compound: LPV	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	35 nM Compound: LPV	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	2.8 nM Compound: LPV	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]
HEK-293T	EC₅₀	160 nM Compound: lopinavir	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	27.8 μM Compound: LPV	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
Huh-7	CC₅₀	>37.6 μM Compound: 6a	Cytotoxicity against human Huh-7 cells incubated for 1 hr by MTS assay Cytotoxicity against human Huh-7 cells incubated for 1 hr by MTS assay	[PMID: 32845145]
MDCK-II	IC₅₀	10.3 μM Compound: LPV	Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells	[PMID: 17664327]
MT2	CC₅₀	>100 μM Compound: lopinavir, LPV	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	0.0026 μM Compound: lopinavir, LPV	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	0.0049 μM Compound: lopinavir, LPV	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	0.007 μM Compound: lopinavir, LPV	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	0.032 μM Compound: LPV	Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay	[PMID: 18955518]
MT2	EC₅₀	4.8 nM Compound: LPV	Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS	[PMID: 19104010]
MT2	CC₅₀	>100 μM Compound: LPV	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	0.028 μM Compound: LPV	Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	EC₅₀	0.035 μM Compound: LPV	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	0.039 μM Compound: LPV	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	CC₅₀	67.9 μM Compound: LPV	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	5.6 nM Compound: LPV	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	EC₅₀	0.1 μM Compound: 6 (ABT-378)	Effective concentration against ritonavir -resistant strains in MT-4 cells. Effective concentration against ritonavir -resistant strains in MT-4 cells.	[PMID: 10669559]
MT4	EC₅₀	0.104 μM Compound: ABT-378 (Lopinavir)	Antiviral activity against HIV in presence of 50% human serum in MT-4 cell was determined Antiviral activity against HIV in presence of 50% human serum in MT-4 cell was determined	[PMID: 11378352]
MT4	EC₅₀	0.1 μM Compound: 1a, ABT-378 Lopinavir	Compound was tested for antiviral activity against HIV-IIIB in MT-4 cells in presence of 50% human serum Compound was tested for antiviral activity against HIV-IIIB in MT-4 cells in presence of 50% human serum	[PMID: 11934584]
MT4	EC₅₀	0.1 μM Compound: 12a (lopinavir)	Antiviral activity against the cytopathic effects of HIV IIIB in MT-4 cells was assayed in the presence of 50% human serum Antiviral activity against the cytopathic effects of HIV IIIB in MT-4 cells was assayed in the presence of 50% human serum	[PMID: 12372511]
MT4	IC₅₀	17.8 μM Compound: 12a (lopinavir)	Cytotoxicity against MT-4 cells Cytotoxicity against MT-4 cells	[PMID: 12372511]
MT4	EC₅₀	0.1 μM Compound: 1a	Tested for cytopathic effect of HIVIIIB in MT-4 cells in presence of 50% human serum Tested for cytopathic effect of HIVIIIB in MT-4 cells in presence of 50% human serum	[PMID: 15109669]
MT4	ED₅₀	0.01 μM Compound: Lopinavir	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	40 nM Compound: Lopinavir	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	400 nM Compound: Lopinavir	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: Lopinavir	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	40 nM Compound: lopinavir	Antiviral activity against HIV1 HXB2 in MT4 cells Antiviral activity against HIV1 HXB2 in MT4 cells	[PMID: 16458505]
MT4	IC₅₀	400 nM Compound: lopinavir	Antiviral activity against HIV1 EP13 in MT4 cells Antiviral activity against HIV1 EP13 in MT4 cells	[PMID: 16458505]
MT4	IC₅₀	>1000 nM Compound: lopinavir	Antiviral activity against HIV D545701 in MT4 cells Antiviral activity against HIV D545701 in MT4 cells	[PMID: 16458505]
MT4	EC₅₀	0.024 μM Compound: lopinavir, LPV	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	0.031 μM Compound: lopinavir, LPV	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	0.033 μM Compound: lopinavir, LPV	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	0.034 μM Compound: lopinavir, LPV	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: lopinavir, LPV	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	0.16 μM Compound: lopinavir, LPV	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	0.19 μM Compound: lopinavir, LPV	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	0.23 μM Compound: lopinavir, LPV	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	0.26 μM Compound: lopinavir, LPV	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	0.27 μM Compound: lopinavir, LPV	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	0.31 μM Compound: lopinavir, LPV	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	15 nM Compound: LPV	Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 1 passage Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 1 passage	[PMID: 17576848]
MT4	EC₅₀	15 nM Compound: LPV	Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 17576848]
MT4	EC₅₀	18 nM Compound: LPV	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	515 nM Compound: LPV	Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 18 passages Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 18 passages	[PMID: 17576848]
MT4	EC₅₀	6 nM Compound: LPV	Antiviral activity against HIV2 MS infected in human MT4 cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay Antiviral activity against HIV2 MS infected in human MT4 cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay	[PMID: 17576848]
MT4	CC₅₀	28 μM Compound: LPV	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	0.019 μM Compound: LPV	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	0.01 μM Compound: LPV, lopinavir	Antiviral activity against HIV1 infected MT4 cells by MTT method Antiviral activity against HIV1 infected MT4 cells by MTT method	[PMID: 17696512]
MT4	EC₅₀	1057 nM Compound: LPV	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	151 nM Compound: LPV	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	18 nM Compound: LPV	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	EC₅₀	30 nM Compound: LPV	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	32 nM Compound: LPV	Antiviral activity against wild-type HIV1 RF 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 RF 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	EC₅₀	3790 nM Compound: LPV	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	>10000 nM Compound: LPV	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]
MT4	EC₅₀	>1 μM Compound: LPV	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	0.018 μM Compound: LPV	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	0.025 μM Compound: LPV	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	0.11 μM Compound: LPV	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	0.14 μM Compound: LPV	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	0.14 μM Compound: LPV	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	0.29 μM Compound: LPV	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	0.3 μM Compound: LPV	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	0.7 μM Compound: LPV	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	1057 nM Compound: LPV	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	152 nM Compound: LPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay in presence of 50% human serum Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay in presence of 50% human serum	[PMID: 19323562]
MT4	EC₅₀	18 nM Compound: LPV	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	3790 nM Compound: LPV	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	>10000 nM Compound: LPV	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	0.016 μM Compound: Lopinavir	Antiviral activity against HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 19954246]
MT4	EC₅₀	0.03 μM Compound: Lopinavir	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 19954246]
MT4	EC₅₀	0.385 μM Compound: Lopinavir	Antiviral activity against indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 19954246]
MT4	EC₅₀	10 nM Compound: LPV	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	>1 μM Compound: LPV	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: LPV	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	>1 μM Compound: LPV	Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	>1 μM Compound: LPV	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	0.037 μM Compound: LPV	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	0.046 μM Compound: LPV	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	0.12 μM Compound: LPV	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	0.19 μM Compound: LPV	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: LPV	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	0.33 μM Compound: LPV	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	IC₅₀	0.035 μM Compound: Lopinavir	Cytotoxicity against human MT4 cells after 5 days by XTT assay Cytotoxicity against human MT4 cells after 5 days by XTT assay	[PMID: 21741133]
MT4	EC₅₀	152 nM Compound: LPV	Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay in presence of 50% human serum Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay in presence of 50% human serum	[PMID: 21899332]
MT4	EC₅₀	18 nM Compound: LPV	Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay	[PMID: 21899332]
MT4	CC₅₀	>10 μM Compound: Lopinavir	Cytotoxicity against human MT4 cells Cytotoxicity against human MT4 cells	[PMID: 23177258]
MT4	EC₅₀	110 nM Compound: Lopinavir	Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 23177258]
MT4	EC₅₀	13 nM Compound: Lopinavir	Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 23177258]
MT4	EC₅₀	310 nM Compound: Lopinavir	Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 23177258]
MT4	EC₅₀	32 nM Compound: Lopinavir	Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 23177258]
MT4	EC₅₀	63 nM Compound: Lopinavir	Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication in presence of 50% human plasma Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication in presence of 50% human plasma	[PMID: 23177258]
MT4	CC₅₀	9.8 μM Compound: lopinavir	Cytotoxicity against human MT4 cells Cytotoxicity against human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	114.6 nM Compound: lopinavir	Antiviral activity against Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant infected in human MT4 cells Antiviral activity against Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant infected in human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	13.2 nM Compound: lopinavir	Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	307.3 nM Compound: lopinavir	Antiviral activity against Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant infected in human MT4 cells Antiviral activity against Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant infected in human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	32.1 nM Compound: lopinavir	Antiviral activity against Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant infected in human MT4 cells Antiviral activity against Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant infected in human MT4 cells	[PMID: 24900331]
MT4	EC₅₀	63.2 nM Compound: lopinavir	Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells in presence of 50% human serum Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells in presence of 50% human serum	[PMID: 24900331]
PBMC	EC₅₀	15 nM Compound: LPV	Antiviral activity against HIV2 MS infected in human PBMC cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay Antiviral activity against HIV2 MS infected in human PBMC cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay	[PMID: 17576848]
PBMC	EC₅₀	>1 μM Compound: LPV	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	>1 μM Compound: LPV	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	>1 μM Compound: LPV	Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	>1 μM Compound: LPV	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	>1 μM Compound: LPV	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	0.034 μM Compound: LPV	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	0.26 μM Compound: LPV	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	>0.16 μM Compound: 6; LPV	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	>0.3 μM Compound: 6; LPV	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	>0.36 μM Compound: 6; LPV	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	>0.38 μM Compound: 6; LPV	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	>0.4365 μM Compound: 6; LPV	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	>0.7 μM Compound: 6; LPV	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: 6; LPV	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	0.007 μM Compound: 6; LPV	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	>1000 nM Compound: 6; LPV	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]
Vero	CC₅₀	>50 μM Compound: Lopinavir	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	9.12 μM Compound: Lopinavir	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
Vero C1008	CC₅₀	>32 μM Compound: 6a	Cytotoxicity against African green monkey Vero E6 cells incubated for 3 days by the MTS assay Cytotoxicity against African green monkey Vero E6 cells incubated for 3 days by the MTS assay	[PMID: 32845145]
Vero C1008	EC₅₀	26.1 μM Compound: 11	Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in viral replication measured after 48 hrs by qRT-PCR assay Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in viral replication measured after 48 hrs by qRT-PCR assay	[PMID: 33486200]

In Vitro

HIV-1 protease is an essential enzyme for production of mature, infective virus^[1].
Lopinavir potently inhibits wild-type and mutant HIV protease (K_i= 1.3 to 3.6 pM), blocks the replication HIV type 1 (EC₅₀=0.006 to 0.017 μM), and maintains high potency against mutant HIV selected by Ritonavir in vivo (EC₅₀=≤0.06 μM)^[2].

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

In Vivo

Coadministration with low-dose Ritonavir significantly improves the pharmacokinetic properties and hence the activity of Lopinavir against HIV-1 protease^[1].

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

Essai clinique

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

Chemical Information

CAS No. 192725-17-0
Appearance Solid
Masse moléculaire 628.80
Formule C₃₇H₄₈N₄O₅
Color White to off-white
SMILES

CC1=C(OCC(N[C@@H](CC2=CC=CC=C2)[C@@H](O)C[C@H](CC3=CC=CC=C3)NC([C@H](C(C)C)N4C(NCCC4)=O)=O)=O)C(C)=CC=C1
Synonyms

ABT-378
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (20)

All In Vivo Efficacy StudyHistological Imaging/StainingIFCell Proliferation/Viability AssayWB

Sort by:

Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
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
Cancer Cell

In vivo models of subclonal oncogenesis and dependency in hematopoietic malignancy. [Abstract]

2024 Nov 11;42(11):1955-1969.e7. PMID: 39532065
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
Bone Res

AIDS patients suffer higher risk of advanced knee osteoarthritis progression due to lopinavir-induced Zmpste24 inhibition. [Abstract]

2025 Jun 3;13(1):58. PMID: 40461512

Lopinavir purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 3;13(1):58. [Abstract]

Lopinavir (100 or 200 mg/kg)/ritonavir (25 or 50 mg/kg) i.p., every 2 days for 28 days) aggravated osteophyte formation in the DMM model.

Lopinavir purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 3;13(1):58. [Abstract]

Lopinavir (100 or 200 mg/kg)/ritonavir (25 or 50 mg/kg, i.p., every 2 days for 28 days) aggravated cartilage erosion and synovitis in the DMM model.

Lopinavir purchased from MedChemExpress. Usage Cited in: Bone Res. 2025 Jun 3;13(1):58. [Abstract]

Lopinavir (100 or 200 mg/kg)/ritonavir (25 or 50 mg/kg, i.p., every 2 days for 28 days) decreased the proportion of Sox9-positive cells from 36% to 18% and increased the proportion of p21-positive cells from 32% to 60%.
Adv Sci (Weinh)

The Compromised Fanconi Anemia Pathway in Prelamin A-Expressing Cells Contributes to Replication Stress-Induced Genomic Instability. [Abstract]

2024 Jun 18:e2307751. PMID: 38894550
Nucleic Acids Res

COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]

2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390
Fundam Res

Tailoring combinational therapy with Monte Carlo method-based regression modeling. [Abstract]

2023 Apr 7;5(6):2975-2982. PMID: 41467005
J Photochem Photobiol A Chem

2025 Nov 15;473:116930.
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
Antiviral Res

HIV protease inhibitor attenuated astrocyte autophagy involvement in inflammation via p38 MAPK pathway. [Abstract]

2022 Dec:208:105463. PMID: 36372295

Lopinavir purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2022 Dec:208:105463. [Abstract]

Lopinavir (LPV) (1, 5, 10, 20, 50 µM; 12, 24, 36, 48 h) inhibits the growth of U87 cells.

Lopinavir purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2022 Dec:208:105463. [Abstract]

Lopinavir (LPV) (0, 1, 5, 10, 20 μM; 24 h) inhibits autophagy in U87 cells in a dose-dependent manner.
Antiviral Res

Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro. [Abstract]

2020 Jun;178:104786. PMID: 32251767
Viruses

Broad-Spectrum Host-Based Antivirals Targeting the Interferon and Lipogenesis Pathways as Potential Treatment Options for the Pandemic Coronavirus Disease 2019 (COVID-19). [Abstract]

2020 Jun 10;12(6):628. PMID: 32532085
J Chem

2025 Oct 15.
Biochem Biophys Res Commun

HIV protease inhibitors block parasite signal peptide peptidases and prevent growth of Babesia microti parasites in erythrocytes. [Abstract]

2019 Sep 10;517(1):125-131. PMID: 31311649
Microbe

2025 Oct 14.
bioRxiv

2024 Feb 3.
Universidade de São Paulo

2020 Sep.
University of Oxford

2019 Jul.

Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (397.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.5903 mL

7.9517 mL

15.9033 mL

5 mM

0.3181 mL

1.5903 mL

3.1807 mL

10 mM

0.1590 mL

0.7952 mL

1.5903 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 90% Corn Oil

Solubility: ≥ 25 mg/mL (39.76 mM); Clear solution

This protocol yields a clear solution of ≥ 25 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 (250.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (3.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: Corn Oil

Solubility: 20 mg/mL (31.81 mM); Suspended solution; Need ultrasonic

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
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- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 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)
Instruction de manipulation (2659 KB)

Références

[1]. Cvetkovic RS, et al. Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs. 2003;63(8):769-802. [Content Brief]

[2]. Sham HL, et al. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998;42(12):3218-3224. [Content Brief]

[3]. 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5903 mL	7.9517 mL	15.9033 mL	39.7583 mL
	5 mM	0.3181 mL	1.5903 mL	3.1807 mL	7.9517 mL
	10 mM	0.1590 mL	0.7952 mL	1.5903 mL	3.9758 mL
	15 mM	0.1060 mL	0.5301 mL	1.0602 mL	2.6506 mL
	20 mM	0.0795 mL	0.3976 mL	0.7952 mL	1.9879 mL
	25 mM	0.0636 mL	0.3181 mL	0.6361 mL	1.5903 mL
	30 mM	0.0530 mL	0.2651 mL	0.5301 mL	1.3253 mL
	40 mM	0.0398 mL	0.1988 mL	0.3976 mL	0.9940 mL
	50 mM	0.0318 mL	0.1590 mL	0.3181 mL	0.7952 mL
	60 mM	0.0265 mL	0.1325 mL	0.2651 mL	0.6626 mL
	80 mM	0.0199 mL	0.0994 mL	0.1988 mL	0.4970 mL
	100 mM	0.0159 mL	0.0795 mL	0.1590 mL	0.3976 mL

Keywords

Lopinavir

20 Cited Publications

100 mg Obtenir un devis

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Lopinavir

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

FDA Approved & Pharmacopeial Drug Library

Targeted Diversity Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Protease Inhibitor Library

Mitochondrial Toxicity Compound Library

Highly Selective Inhibitors 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

Publications Citing Use of MedChemExpress (MCE) Lopinavir

Voir tous les produits spécifiques à Isoform HIV

Activité biologique

Chemical Information

Publications (20)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Lopinavir

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

FDA Approved & Pharmacopeial Drug Library

Targeted Diversity Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Protease Inhibitor Library

Mitochondrial Toxicity Compound Library

Highly Selective Inhibitors 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

Publications Citing Use of MedChemExpress (MCE) Lopinavir

Voir tous les produits spécifiques à Isoform HIV

Activité biologique

Chemical Information

Publications (20)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Lopinavir Related Classifications

Cat. No.: HY-14588