Description
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.
Product information
CAS Number: 1428327-31-4
Molecular Weight: 488.64
Formula: C28H32N4O2S
Chemical Name: N-{[4-(4-phenylpiperazin-1-yl)oxan-4-yl]methyl}-2-(phenylsulfanyl)pyridine-3-carboxamide
Smiles: O=C(NCC1(CCOCC1)N1CCN(CC1)C1C=CC=CC=1)C1=CC=CN=C1SC1C=CC=CC=1
InChiKey: XREFXUCWSYMIOG-UHFFFAOYSA-N
InChi: InChI=1S/C28H32N4O2S/c33-26(25-12-7-15-29-27(25)35-24-10-5-2-6-11-24)30-22-28(13-20-34-21-14-28)32-18-16-31(17-19-32)23-8-3-1-4-9-23/h1-12,15H,13-14,16-22H2,(H,30,33)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (204.65 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
JNJ-47965567 exhibits high affinity for human and rat P2X7 in membrane preparations of 1321N1 cells. 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. 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.
In Vivo:
JNJ-47965567 (30-100 mg/kg; s.c.) attenuates IL-1β release induced by Bz-ATP. JNJ-47965567 (30 mg/kg) attenuates amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.