| Identification | Back Directory | [Name]
(r)-(2-chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyrimidin-2-yl)-4-methyl-1,4,6,7-tetrahydro-5h-[1,2,3]triazolo[4,5-c]pyridin-5-yl)methanone | [CAS]
1627902-21-9 | [Synonyms]
(r)-(2-chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyrimidin-2-yl)-4-methyl-1,4,6,7-tetrahydro-5h-[1,2,3]triazolo[4,5-c]pyridin-5-yl)methanone
Methanone, [2-chloro-3-(trifluoromethyl)phenyl][(4R)-1-(5-fluoro-2-pyrimidinyl)-1,4,6,7-tetrahydro-4-methyl-5H-1,2,3-triazolo[4,5-c]pyridin-5-yl]- | [Molecular Formula]
C18H13ClF4N6O | [MDL Number]
MFCD31556312 | [MOL File]
1627902-21-9.mol | [Molecular Weight]
440.78 |
| Chemical Properties | Back Directory | [Boiling point ]
635.6±65.0 °C(Predicted) | [density ]
1.62±0.1 g/cm3(Predicted) | [solubility ]
DMSO:62.5(Max Conc. mg/mL);141.79(Max Conc. mM) | [form ]
Solid | [pka]
-1.93±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively. | [in vivo]
JNJ-54175446 shows dose-dependent occupancy with the ED50 of 0.46 mg/kg, corresponding to plasma EC50 of 105 ng/mL[1]. | [IC 50]
P2X7 Receptor | [References]
[1] Letavic MA, et al. 4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate. Send to DOI:10.1021/acs.jmedchem.7b00408 |
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