Saquinavir (Synonyms: Ro 31-8959)

Name: Saquinavir
Brand: MedChemExpress
SKU: HY-17007
Rating: 5.0 (11 reviews)

Cat. No.: HY-17007 Purity: 99.73%: FAQs
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Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.36 μM.

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

Saquinavir Chemical Structure

CAS No. : 127779-20-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 252	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 396	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Saquinavir:

10 Publications Citing Use of MCE Saquinavir

: Saquinavir purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2022 Nov 10;105463. [Abstract]; Saquinavir (1, 5, 10, 20 µM; 24 h) inhibits the autophagy in U87 cells, and the expression of p62 is increased in a concentrationdependent manner.

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Biological Activity
Purity & Documentation
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Customer Review

Description

Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.36 μM.

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	EC₅₀	0.2 nM Compound: SQV	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	0.2 nM Compound: SQV	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	IC₅₀	2 nM Compound: Ro-318959	Antiviral activity in HIV-infected CEM cells using whole cell assay Antiviral activity in HIV-infected CEM cells using whole cell assay	10.1016/0960-894X(95)00102-Y
CCRF-CEM	EC₅₀	2.2 nM Compound: SQV	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	3.6 nM Compound: SQV	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]
CEM-SS	CC₅₀	> 1 x 10^-5 M Compound: Saquinavir	Cytotoxicity against human CEM-SS cells after 5 days by MTT assay Cytotoxicity against human CEM-SS cells after 5 days by MTT assay	[PMID: 17950955]
CEM-SS	IC₅₀	9 nM Compound: Saquinavir	Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as reverse transcriptase activity after 5 days by MTT assay Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as reverse transcriptase activity after 5 days by MTT assay	[PMID: 17950955]
CHO	IC₅₀	1.9 μM Compound: saquinavir	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
H9	IC₅₀	20 nM Compound: Ro-318959	Tested for the inhibitory activity against HIV-1 in H-9 cell lines assessed by syncytium formation and reverse transcriptase assay Tested for the inhibitory activity against HIV-1 in H-9 cell lines assessed by syncytium formation and reverse transcriptase assay	10.1016/0960-894X(95)00306-E
HEK293	EC₅₀	1.8 nM Compound: SQV	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	12 nM Compound: saquinavir	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]
Hepatocyte	IC₅₀	35.2 nM Compound: Saquinavir	Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs	[PMID: 18212104]
HepG2	CC₅₀	12.4 μM Compound: Saquinavir	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
LLC-PK1	IC₅₀	> 50 μM Compound: Saquinavir	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	> 50 μM Compound: Saquinavir	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	12 μM Compound: Saquinavir	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
MT2	EC₅₀	0.003 μM Compound: saquinavir, SQV	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	0.0043 μM Compound: saquinavir, SQV	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: saquinavir, SQV	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	0.014 μM Compound: SQV	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	IC₅₀	0.015 μM Compound: SQV	Antiviral activity against HIV1 LAI infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 21194227]
MT2	EC₅₀	13.6 nM Compound: Saquinavir	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	15 nM Compound: SQV	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	16.4 μM Compound: saquinavir, SQV	Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	CC₅₀	32.3 μM Compound: Saquinavir	Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay	10.1039/C1MD00147G
MT2	CC₅₀	9.9 μM Compound: SQV	Cytotoxicity against human MT2 cells by MTT assay Cytotoxicity against human MT2 cells by MTT assay	[PMID: 18955518]
MT4	CC₅₀	> 1 x 10^-5 M Compound: Saquinavir	Cytotoxicity against human MT4 cells after 4 days by MTT assay Cytotoxicity against human MT4 cells after 4 days by MTT assay	[PMID: 17950955]
MT4	EC₅₀	> 1 μM Compound: SQV	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	> 1 μM Compound: SQV	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	> 1 μM Compound: saquinavir, SQV	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	0.003 μM Compound: SQV	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	0.005 μM Compound: SQV	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	0.007 μM Compound: saquinavir, SQV	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	0.008 μM Compound: SQV	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	0.008 μM Compound: SQV	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	0.01 μM Compound: SQV	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	0.01 μM Compound: SQV	Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.01 μM Compound: SQV	Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.01 μM Compound: SQV	Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.01 μM Compound: SQV	Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.01 μM Compound: SQV	Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.01 μM Compound: SQV, saquinavir	Antiviral activity against HIV1 infected MT4 cells by MTT method Antiviral activity against HIV1 infected MT4 cells by MTT method	[PMID: 17696512]
MT4	EC₅₀	0.01 μM Compound: SQV	Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay	[PMID: 17548498]
MT4	EC₅₀	0.01 μM Compound: saquinavir, SQV	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	0.012 μM Compound: SQV	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	0.012 μM Compound: saquinavir, SQV	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	0.016 μM Compound: SQV	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	0.02 μM Compound: SQV	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.02 μM Compound: SQV	Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.02 μM Compound: SQV	Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.02 μM Compound: SQV	Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in	[PMID: 24805780]
MT4	EC₅₀	0.02 μM Compound: SQV	Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.022 μM Compound: SQV	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	0.022 μM Compound: saquinavir, SQV	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	0.024 μM Compound: saquinavir, SQV	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	0.026 μM Compound: SQV	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	0.028 μM Compound: SQV	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	0.028 μM Compound: SQV	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	0.031 μM Compound: SQV	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	0.031 μM Compound: saquinavir, SQV	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	0.032 μM Compound: saquinavir, SQV	Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.032 μM Compound: saquinavir, SQV	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	0.033 μM Compound: SQV	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	0.034 μM Compound: SQV	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	0.037 μM Compound: saquinavir, SQV	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	0.059 μM Compound: saquinavir, SQV	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	0.09 μM Compound: SQV	Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	10 nM Compound: SQV	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	12 nM Compound: SQV	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	CC₅₀	15 μM Compound: SQV	Cytotoxicity against human MT4 cells after 96 hrs by MTT assay Cytotoxicity against human MT4 cells after 96 hrs by MTT assay	[PMID: 24805780]
MT4	IC₅₀	18 nM Compound: Saquinavir	Antiviral activity against HTLV1 3B infected in human MT4 cells assessed as reverse transcriptase activity after 5 days by MTT assay Antiviral activity against HTLV1 3B infected in human MT4 cells assessed as reverse transcriptase activity after 5 days by MTT assay	[PMID: 17950955]
MT4	CC₅₀	19 μM Compound: SQV	Cytotoxicity against human MT4 cells after 6 days by MTT assay Cytotoxicity against human MT4 cells after 6 days by MTT assay	[PMID: 17638694]
MT4	CC₅₀	26 μM Compound: SQV	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 17548498]
MT4	EC₅₀	5 nM Compound: SQV	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]
Oocyte	IC₅₀	13 μM Compound: Saquinavir	Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes assessed as reduction in [3H]-chloroquine uptake after 1.5 to 2 hrs Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes assessed as reduction in [3H]-chloroquine uptake after 1.5 to 2 hrs	[PMID: 23145816]
PBMC	EC₅₀	0.004 μM Compound: 1; SQV	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	0.008 μM Compound: SQV	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	0.03 μM Compound: SQV	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	0.032 μM Compound: SQV	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	0.033 μM Compound: 1; SQV	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	0.035 μM Compound: 1; SQV	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	0.1 μM Compound: 1; SQV	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	0.11 μM Compound: 1; SQV	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	0.19 μM Compound: SQV	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	0.26 μM Compound: SQV	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	0.27 μM Compound: 1; SQV	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	0.27 μM Compound: SQV	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	0.29 μM Compound: 1; SQV	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	0.3 μM Compound: SQV	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	CC₅₀	78 μM Compound: SQV	Cytotoxicity against human PHA-PBMC cells by MTT assay Cytotoxicity against human PHA-PBMC cells by MTT assay	[PMID: 17548498]
SUP-T1	IC₅₀	20 nM Compound: Ro-318959	Tested for the inhibitory activity against HIV-1 in Sup T1 cell lines assessed by syncytium formation and reverse transcriptase assay Tested for the inhibitory activity against HIV-1 in Sup T1 cell lines assessed by syncytium formation and reverse transcriptase assay	10.1016/0960-894X(95)00306-E

In Vitro

Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. HIV protease is vital for both viral replication within the cell and release of mature viral particles from an infected cell. Saquinavir binds to the active site of the viral protease and prevents cleavage of viral polyproteins, preventing maturation of the virus. Saquinavir inhibits both HIV-1 and HIV-2 proteases.Studies have also looked at Saquinavir as a possible anti-cancer agent.

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

Clinical Trial

Molecular Weight

670.84

Formula

C₃₈H₅₀N₆O₅

CAS No.

127779-20-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@@H](CC(N)=O)C(N[C@@H](CC1=CC=CC=C1)[C@H](O)CN2[C@H](C(NC(C)(C)C)=O)C[C@@](CCCC3)([H])[C@@]3([H])C2)=O)C4=NC5=CC=CC=C5C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (149.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4907 mL	7.4533 mL	14.9067 mL
5 mM	0.2981 mL	1.4907 mL	2.9813 mL
10 mM	0.1491 mL	0.7453 mL	1.4907 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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (3.73 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 (3.73 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.73%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (252 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[1]. Marco Donia, Danijela Maksimovic-Ivanic, Sanja Mijatovic, et al. In vitro and in vivo anticancer action of Saquinavir-NO, a novel nitric oxide-derivative of the protease inhibitor saquinavir, on hormone resistant prostate cancer cells. Cell cycle. 2011, 1

[2]. Walmsley Sharon, Avihingsanon Anchalee, Slim Jihad et al. Gemini: A Noninferiority Study of Saquinavir/Ritonavir Versus Lopinavir/Ritonavir as Initial HIV-1 Therapy in Adults. JAIDS Journal of Acquired Immune Deficiency Syndromes. 2009,50 (4) :367-374.

[3]. Saquinavir

[4]. Barillari Giovannia, Iovane Andréa, Bacigalupo Ilariaa, et al. Ritonavir or saquinavir impairs the invasion of cervical intraepithelial neoplasia cells via a reduction of MMP expression and activity. AIDS. 2012, 26 (8): 909-919.

[5]. Martha Stefanidou, Carolina Herrera, Naomi Armanasco et al. Saquinavir Inhibits Early Events Associated with Establishment of HIV-1 Infection: Potential Role for Protease Inhibitors in Prevention. Antimicrob. Agents Chemother. 2012, 56 (8): 4381-4390.

[6]. 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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.4907 mL	7.4533 mL	14.9067 mL	37.2667 mL
	5 mM	0.2981 mL	1.4907 mL	2.9813 mL	7.4533 mL
	10 mM	0.1491 mL	0.7453 mL	1.4907 mL	3.7267 mL
	15 mM	0.0994 mL	0.4969 mL	0.9938 mL	2.4844 mL
	20 mM	0.0745 mL	0.3727 mL	0.7453 mL	1.8633 mL
	25 mM	0.0596 mL	0.2981 mL	0.5963 mL	1.4907 mL
	30 mM	0.0497 mL	0.2484 mL	0.4969 mL	1.2422 mL
	40 mM	0.0373 mL	0.1863 mL	0.3727 mL	0.9317 mL
	50 mM	0.0298 mL	0.1491 mL	0.2981 mL	0.7453 mL
	60 mM	0.0248 mL	0.1242 mL	0.2484 mL	0.6211 mL
	80 mM	0.0186 mL	0.0932 mL	0.1863 mL	0.4658 mL
	100 mM	0.0149 mL	0.0745 mL	0.1491 mL	0.3727 mL

Saquinavir Related Classifications

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.

Keywords:

Saquinavir127779-20-8Ro 31-8959HIVHIV ProteaseSARS-CoVHuman immunodeficiency virusSARS coronavirusInhibitorinhibitorinhibit

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Saquinavir (Synonyms: Ro 31-8959)

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