INCB9471

Research use only, not for human use.

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

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.

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INCB 9471 | INCB-9471

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Infection

HIV Infection

869769-98-2

559.678

C30H40F3N5O2

>98% (HPLC)

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

(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

(-20℃)

With Ice Pack

≥ 2 years