2166558-11-6
2166558-11-6 structure
- Name: JNJ-55308942
- Chemical Name: JNJ-55308942
- CAS Number: 2166558-11-6
- Molecular Formula: C17H12F5N7O
- Molecular Weight: 425.323
- Create Date: 2020-01-11 19:29:51
- Modify Date: 2023-01-12 14:34:56
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JNJ-55308942 is a novel highly potent P2X7 antagonist with Ki of 1.0 and 6.5 nM for rat and human hP2X7, demonstrates significant activity against a panel of related P2X receptors (P2X1, P2X2, P2X3, P2X2/3, and P2X4; also shows insignificant inhibition of nine CYP isoforms (IC50>15 uM); exhibits excellent P2X7 receptor occupancy in the hippocampus of rats with low ED50 of 0.07 mg/kg and unbound plasma EC50 of 12 ng/mL, suppresses brain IL-1β release in vivo in freely moving rats challenged with the P2X7 agonist Bz-ATP; possesses good tolerability margins in preclinical species, as well as an acceptable cardiovascular safety profile in vivo. Epilepsy Phase 1 Clinical
| Name | JNJ-55308942 |
|---|
| Description | JNJ-55308942 is a novel highly potent P2X7 antagonist with Ki of 1.0 and 6.5 nM for rat and human hP2X7, demonstrates significant activity against a panel of related P2X receptors (P2X1, P2X2, P2X3, P2X2/3, and P2X4; also shows insignificant inhibition of nine CYP isoforms (IC50>15 uM); exhibits excellent P2X7 receptor occupancy in the hippocampus of rats with low ED50 of 0.07 mg/kg and unbound plasma EC50 of 12 ng/mL, suppresses brain IL-1β release in vivo in freely moving rats challenged with the P2X7 agonist Bz-ATP; possesses good tolerability margins in preclinical species, as well as an acceptable cardiovascular safety profile in vivo. Epilepsy Phase 1 Clinical |
|---|---|
| References | References 1. Chrovian CC, et al. J Med Chem. 2018 Jan 11;61(1):207-223. View Related Products by Target P2X Receptor Epilepsy |
| Molecular Formula | C17H12F5N7O |
|---|---|
| Molecular Weight | 425.323 |
| Storage condition | -20°C |