INCB9471 |CAS:869769-98-2 Probechem Biochemicals

Chemical Structure : INCB9471

INCB9471 (INCB 9471;INCB-9471)

Catalog No.: PC-60672Not For Human Use, Lab Use Only.

INCB9471 is a potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs.

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Biological Activity

INCB9471 is a potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs.
INCB9471 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.
INCB9471 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.
INCB9471 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.

Physicochemical Properties

M.Wt	559.678
Formula	C30H40F3N5O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

References

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.

INCB9471 (INCB 9471;INCB-9471)

Biological Activity

Physicochemical Properties

References

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