JNJ-42253432
- CAS NO.:1428327-35-8
- Empirical Formula: C28H38N4O
- Molecular Weight: 446.63
- Update Date: 2026-01-31 10:02:37
What is JNJ-42253432?
Biological Activity
JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively[1]. When dosed in rats, JNJ-42253432 occupied the brain P2X7 channel with an ED50 of 0.3 mg/kg, corresponding to a mean plasma concentration of 42 ng/ml. JNJ-42253432 also increased serotonin levels in the rat brain, which is due to antagonism of the serotonin transporter (SERT) resulting in an ED50 of 10 mg/kg for SERT occupancy[1].
References
[1]. Brian Lord, et al. Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41.
Properties of JNJ-42253432
| Boiling point: | 592.8±50.0 °C(Predicted) |
| Density | 1.130±0.06 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| pka | 16.14±0.20(Predicted) |
| form | Solid |
| color | White to off-white |
Safety information for JNJ-42253432
Computed Descriptors for JNJ-42253432
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