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Chemical Structure : JNJ-55308942
Catalog No.: PC-62763Not For Human Use, Lab Use Only.
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.
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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
| M.Wt | 425.323 | |
| Formula | C17H12F5N7O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Chrovian CC, et al. J Med Chem. 2018 Jan 11;61(1):207-223.
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