Chemical Structure : INCB9471
货号: 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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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.
分子量 | 559.678 | |
分子式 | C30H40F3N5O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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