GSK3532795 (Synonyms: BMS-955176)

Name: GSK3532795
Brand: MedChemExpress
SKU: HY-112714
Rating: 4.5 (0 reviews)

Cat. No.: HY-112714 Pureza: 98.0%: Ficha de datos
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GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC₅₀s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively.

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GSK3532795 Estructura química

No. CAS : 1392312-45-6

Tamaño	Stock	Cantidad
1 mg	En stock	Estimated Time of Arrival: December 31
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Other Forms of GSK3532795:

GSK3532795 oxalate Obtener un presupuesto
GSK3532795 hydrochloride Obtener un presupuesto

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Ver todas las isoformas

HIV HIV-1 HIV-2

Actividad biológica
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Referencias
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Descripciòn

IC₅₀ & Target

HIV-1

Cellular Effect

Cell Line	Type	Value	Description	References
MT2	CC₅₀	13 μM Compound: 3; GSK3532795, BMS-955176	Cytotoxicity against human MT2 cells assessed as reduction in cell viability Cytotoxicity against human MT2 cells assessed as reduction in cell viability	[PMID: 36441509]
MT2	CC₅₀	13 μM Compound: 4; GSK3532795, BMS-955176	Cytotoxicity in human MT2 cells assessed as reduction in cell viability Cytotoxicity in human MT2 cells assessed as reduction in cell viability	[PMID: 36044257]
MT2	CC₅₀	9.2 nM Compound: 2; BMS-955176	Cytotoxicity against human MT2 cells Cytotoxicity against human MT2 cells	[PMID: 27326328]
MT2	CC₅₀	9.2 μM Compound: 1; BMS-955176, GSK3532795	Cytotoxicity against human MT2 cells assessed as reduction in cell viability Cytotoxicity against human MT2 cells assessed as reduction in cell viability	[PMID: 30067361]
MT2	CC₅₀	9.2 μM Compound: 3; GSK3532795; BMS-955176	Cytotoxicity against human MT2 cells Cytotoxicity against human MT2 cells	[PMID: 33508465]
MT2	EC₅₀	1.9 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay	[PMID: 27326328]
MT2	EC₅₀	1.9 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay	[PMID: 27326328]
MT2	EC₅₀	10.2 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum/27 mg/ml human serum albumin by dual-luciferase reporter assay Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum/27 mg/ml human serum albumin by dual-luciferase reporter assay	[PMID: 27326328]
MT2	EC₅₀	13 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay	[PMID: 27326328]
MT2	EC₅₀	2 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay	[PMID: 27326328]
MT2	EC₅₀	2.7 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay	[PMID: 27326328]
MT2	EC₅₀	2.8 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay	[PMID: 27326328]
MT2	EC₅₀	3.6 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay	[PMID: 27326328]
MT2	EC₅₀	3.9 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation Binding affinity to gag polyprotein in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation	[PMID: 27326328]
MT2	EC₅₀	4.5 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay	[PMID: 27326328]
MT2	EC₅₀	7.3 nM Compound: 2; BMS-955176	Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay	[PMID: 27326328]

In Vitro

GSK3532795 exhibits K_ds of 3.2 ± 0.6, 4.3 ± 2.0, 6.5 ± 2.2 and 33.6 ± 5.9 nM for HIV WT, HIV V362I, HIV V370A, HIV ΔV370, respectively^[1].

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

Ensayo clínico

Peso molecular

691.02

Fòrmula

C₄₂H₆₂N₂O₄S

No. CAS

1392312-45-6

Appearance

Solid

Color

White to off-white

SMILES

CC1(C)C(C2=CC=C(C(O)=O)C=C2)=CC[C@@]3(C)[C@@]1([H])CC[C@]4(C)[C@]3([H])CC[C@@]5([H])[C@@]4(C)CC[C@]6(NCCN7CCS(CC7)(=O)=O)[C@]5([H])[C@H](C(C)=C)CC6

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Pureza y Documentación

Purity: 99.59%

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Ficha de datos (269 KB) SDS (252 KB)

COA (250 KB) HNMR (278 KB) LCMS (259 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Regueiro-Ren A, et al. Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176). J Med Chem. 2018 Aug 23;61(16):7289-7313. [Content Brief]

GSK3532795 Related Classifications

Infection

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The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

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

Keywords:

GSK35327951392312-45-6BMS-955176GSK 3532795GSK-3532795BMS955176BMS 955176HIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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GSK3532795 (Synonyms: BMS-955176)

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Other Forms of GSK3532795:

GSK3532795 Related Antibodies

Recomendaciones destacadas

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas HIV:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

GSK3532795 Related Antibodies

GSK3532795 Related Classifications

Calculadora de molaridad

Calculadora de dilución

The molarity calculator equation

The dilution calculator equation

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