PF-05105679 |
| カタログ番号GC46199 |
PF-05105679 は、IC50 が 103 nM の経口活性および選択的 TRPM8 アンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1398583-31-7
Sample solution is provided at 25 µL, 10mM.
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PF-05105679 is an antagonist of transient receptor potential melastatin 8 (TRPM8; IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor).1 It is greater than 100-fold selective for TRPM8 over a panel of 90 receptors, ion channels, and enzymes. PF-05105679 inhibits calcium flux induced by cold or the TRPM8 agonist WS-12 in HEK293 cells expressing the human TRPM8 (IC50s = 480 and 181 nM, respectively). Intravenous infusion of PF-05105679 (46.67 μg/kg per minute) reverses cold-induced reductions in bladder capacity in anesthetized guinea pigs. It decreases the core body temperature in rats when administered at doses of 100 and 300 mg/kg.
|1. Winchester, W.J., Gore, K., Glatt, S., et al. Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J. Pharmacol. Exp. Ther. 351(2), 259-269 (2014).
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