| Bioactivity | 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. | ||||||||||||
| Target | pIC50: 8.46 (hP2X7 receptor), 8.81 (rP2X7 receptor) | ||||||||||||
| Invitro | JNJ-54175446 (Compound 14) is a potent and selective brain penetrant P2X7 antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 and rP2X7, respectively. JNJ-54175446 shows less potent activity against mouse, dog and Macaque P2X7 (pIC50, 7.8, 7.9 and 8.1, respectively)[1]. | ||||||||||||
| 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]. | ||||||||||||
| Name | JNJ-54175446 | ||||||||||||
| CAS | 1627902-21-9 | ||||||||||||
| Formula | C18H13ClF4N6O | ||||||||||||
| Molar Mass | 440.78 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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 |
JNJ-54175446
CAS: 1627902-21-9 F: C18H13ClF4N6O W: 440.78
JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7
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