INCB9471

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INCB9471 is a potent, selective and orally active CCR5 antagonist. INCB9471 shows anti-HIV-1 activity.

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

INCB9471 Chemical Structure

CAS No. : 869769-98-2

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Other Forms of INCB9471:

CCR5 antagonist 5 Get quote

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•Related Small Molecules:

•Related Proteins:

View All CCR Isoform Specific Products:

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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HIV HIV-1 HIV-2

Biological Activity
Purity & Documentation
References
Customer Review

Description

INCB9471 is a potent, selective and orally active CCR5 antagonist. INCB9471 shows anti-HIV-1 activity^[1]^[2].

IC₅₀ & Target^[1]^[2]

CCR5

HIV-1

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	0.16 nM Compound: 22a, INCB9471, diastereomer1	Antiviral activity against HIV-1 BaL infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA Antiviral activity against HIV-1 BaL infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA	[PMID: 24900235]
PBMC	IC₅₀	0.36 nM Compound: 22a, INCB9471, diastereomer1	Antiviral activity against HIV-1 ADA infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA Antiviral activity against HIV-1 ADA infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA	[PMID: 24900235]

In Vitro

INCB9471 (0-1 µM) inhibits MIP-1 induced chemotaxis of rhIL-10-treated human monocytes with an IC₅₀ value of 4.8 nM^[1].

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

In Vivo

Pharmacokinetic Parameters^[2].

		rats	dogs
i.v.	dose iv/po (mg/kg)	1/20	1/20
	CL (L/h/kg)	0.62	0.2
	Vd_ss (L/h)	4.1	3.8
	T_1/2 (h)	6	11
	AUC (nM h)	2898	7854
p.o.	T_max (h)	3	0.5
	C_max(ng/mL)	4071	14007
	C_24h (nM)	1088
	T_1/2 (h)	12	17
	AUC (nM h)	55160	149779
	F (%)	100	95

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

Molecular Weight

559.67

Formula

C₃₀H₄₀F₃N₅O₂

CAS No.

869769-98-2

SMILES

CCO[C@H]1[C@H](N2[C@H](CN(C3(CCN(CC3)C(C4=C(C)N=CN=C4C)=O)C)CC2)C)C5=CC=C(C(F)(F)F)C=C5C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Shin N, et al. Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection. J Pharmacol Exp Ther. 2011 Jul;338(1):228-39. [Content Brief]

[2]. Xue CB, et al. Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity. ACS Med Chem Lett. 2010 Aug 25;1(9):483-7. [Content Brief]

INCB9471 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:

INCB9471869769-98-2INCB 9471INCB-9471CCRHIVCC chemokine receptorHuman immunodeficiency virusorally activeanti-HIV-1 activitymonocytesInhibitorinhibitorinhibit

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