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JNJ-47965567

Chemical Structure : JNJ-47965567

CAS No.: 1428327-31-4

JNJ-47965567 (JNJ47965567)

Catalog No.: PC-63425Not For Human Use, Lab Use Only.

JNJ-47965567 is a potent, selective, centrally permeable P2X7 receptor antagonist with pKi of 7.9 and 8.7 for human and rat P2X7, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

JNJ-47965567 is a potent, selective, centrally permeable P2X7 receptor antagonist with pKi of 7.9 and 8.7 for human and rat P2X7, respectively; attenuates IL-1β release with pEC50 of 6.7 (human blood), 7.5 (human monocytes) and 7.1 (rat microglia); exhibits target engagement in rat brain with brain EC50 of 78 ± 19 ng/ml, as well as functional block of Bz-ATP induced IL-1β release; attenuateas amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain.

Physicochemical Properties

M.Wt 488.65
Formula C28H32N4O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[[4-(4-phenylpiperazin-1-yl)oxan-4-yl]methyl]-2-phenylsulfanylpyridine-3-carboxamide

References

1. Bhattacharya A, et al. Br J Pharmacol. 2013 Oct;170(3):624-40.

2. Jimenez-Pacheco A, et al. J Neurosci. 2016 Jun 1;36(22):5920-32.

3. Letavic MA, et al. ACS Med Chem Lett. 2013 Mar 12;4(4):419-22.

4. Rodriguez-Alvarez N, et al. Neuropharmacology. 2017 Apr;116:351-363.

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