869769-98-2
869769-98-2 structure
- Name: INCB9471
- Chemical Name: INCB-9471
- CAS Number: 869769-98-2
- Molecular Formula: C30H40F3N5O2
- Molecular Weight: 559.666
- Create Date: 2020-01-20 09:19:57
- Modify Date: 2024-04-09 17:22:11
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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
| Name | INCB-9471 |
|---|---|
| Synonyms |
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 |
| 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 |
| 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 |