INCB9471

Names

[ Name ]:
INCB9471

[Synonym ]:
C5D4W25708
(4,6-Dimethyl-5-pyrimidinyl)(4-{(3S)-4-[(1R,2R)-2-ethoxy-5-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]-3-methyl-1-piperazinyl}-4-methyl-1-piperidinyl)methanone
Methanone, (4,6-dimethyl-5-pyrimidinyl)[4-[(3S)-4-[(1R,2R)-2-ethoxy-2,3-dihydro-5-(trifluoromethyl)-1H-inden-1-yl]-3-methyl-1-piperazinyl]-4-methyl-1-piperidinyl]-
INCB-9471

Biological Activity

[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

[References]

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. View Related Products by Target Chemokine Receptor (CCR and CXCR) HIV Infection

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
639.2±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₀H₄₀F₃N₅O₂

[ Molecular Weight ]:
559.666

[ Flash Point ]:
340.3±31.5 °C

[ Exact Mass ]:
559.313416

[ LogP ]:
2.63

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.582