Cas No.: | 869769-98-2 |
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 |
Synonyms: | INCB 9471;INCB-9471 |
SMILES: | CCO[C@H]1[C@H](N2[C@@H](C)CN(CC2)C3(C)CCN(CC3)C(=O)C4=C(C)N=CN=C4C)C5=C(C=C(C=C5)C(F)(F)F)C1 |
Formula: | C30H40F3N5O2 |
M.Wt: | 559.678 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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 InfectionPhase 1 Clinical |