| Bioactivity | JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology[1]. | ||||||||||||
| Target | pKi: 7.9 (huaman P2X7), 8.7 (rat P2X7) | ||||||||||||
| Invitro | JNJ-47965567 exhibits high affinity for human and rat P2X7 in membrane preparations of 1321N1 cells[1].JNJ-47965567 does not block IL-6 and TNF-α release, under identical conditions (LPS and BZ-ATP) used for IL-1β and IL-18 release[1].JNJ-47965567 attenuates IL-1β release with pIC50s of 6.7 ± 0.07 (human blood), 7.5 ± 0.07 (human monocytes) and 7.1 ± 0.1 (rat microglia), respectively, in native systems[1]. | ||||||||||||
| In Vivo | JNJ-47965567 (30-100 mg/kg; s.c.) attenuates IL-1β release induced by Bz-ATP[1].JNJ-47965567 (30 mg/kg) attenuates amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain[1]. Animal Model: | ||||||||||||
| Name | JNJ-47965567 | ||||||||||||
| CAS | 1428327-31-4 | ||||||||||||
| Formula | C28H32N4O2S | ||||||||||||
| Molar Mass | 488.64 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Bhattacharya A, et al. Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br J Pharmacol. 2013 Oct;170(3):624-40. |
JNJ-47965567
CAS: 1428327-31-4 F: C28H32N4O2S W: 488.64
JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and
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