INCB9471( INCB 9471 | INCB-9471 )

Catalog No. M16318 CAS No. 869769-98-2

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

INCB9471
Note

Research use only, not for human use.
Brief Description

A potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs.
Description

A potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs; inhibits CCR5-mediated signaling events such as intracellular calcium mobilization, ERK phosphorylation, and CCR5 receptor internalization with IC50 values of 16, 3, and 1.5 nM, respectively; demonstrates anti-HIV-1 activity against R5 HIV-1 strains representing the major clades including A, B, C, D, E, F, G, and J with mean IC50 of 9 nM in PBMCs; also is a potent inhibitor of mutant HIV-1 variants that are resistant to other drugs including NRTIs, NNRTIs, PIs, and the fusion inhibitor T20.HIV Infection Phase 1 Clinical.
In Vitro

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In Vivo

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Synonyms

INCB 9471 | INCB-9471
Pathway

GPCR/G Protein
Target

Chemokine Receptor
Recptor

Chemokine Receptor
Research Area

Infection
Indication

HIV Infection

CAS Number

869769-98-2
Formula Weight

559.678
Molecular Formula

C30H40F3N5O2
Purity

>98% (HPLC)
Solubility

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SMILES

CCOC1CC2=C(C1N3CCN(CC3C)C4(CCN(CC4)C(=O)C5=C(N=CN=C5C)C)C)C=CC(=C2)C(F)(F)F
Chemical Name

(4,6-dimethylpyrimidin-5-yl)(4-((S)-4-((1R,2R)-2-ethoxy-5-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl)-3-methylpiperazin-1-yl)-4-methylpiperidin-1-yl)methanone

1. Xue CB, et al. ACS Med Chem Lett. 2010 Aug 25;1(9):483-7. 2. Shin N, et al. J Pharmacol Exp Ther. 2011 Jul;338(1):228-39.

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