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Chemical Structure : KPR-5714
Catalog No.: PC-72111Not For Human Use, Lab Use Only.
KPR-5714 (KPR5714) is a novel potent, selective TRPM8 antagonist with IC50 of 25.3 and 22.4 nM against hTRPM8 and rTRPM8, respectively.
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KPR-5714 (KPR5714) is a novel potent, selective TRPM8 antagonist with IC50 of 25.3 and 22.4 nM against hTRPM8 and rTRPM8, respectively.
KPR-5714 dispalys 400-fold against human TRPA1, TRPV1, and TRPV4, and does not show inhibitory effects for ASIC1a, ASIC3, Nav1.3, Nav1.5, Nav1.6, Nav1.7, and Nav1.8 (IC50 values >10 uM).
KPR-5714 (i.p.) inhibited the hyperactivity of mechanosensitive C-fibers of bladder afferents and dose-dependently increased the intercontraction interval shortened by intravesical instillation of acetic acid in anesthetized rats.
KPR-5714 (orally administered) dose-dependently increased the mean voided volume and decreased voiding frequency without affecting total voided volume in vivo.
| M.Wt | 474.42 | |
| Formula | C22H18F4N6O2 | |
| Appearance | Solid | |
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1. Nakanishi O, et al. J Pharmacol Exp Ther. 2020 May;373(2):239-247.
2. Aizawa N, et al. Eur J Pharmacol. 2021 May 15;899:173995.
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