A TRPM8 antagonist (IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor); >100-fold selective for TRPM8 over a panel of 90 receptors

PF-05105679 – 10 mg

Brand:
Cayman
CAS:
1398583-31-7
Storage:
-20
UN-No:
- /

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).{52271} 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.  

 

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SKU: 29489 - 10 mg Category:

Description

A TRPM8 antagonist (IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor); >100-fold selective for TRPM8 over a panel of 90 receptors, ion channels, and enzymes; inhibits cold- and WS-12-induced calcium flux in HEK293 cells expressing the human TRPM8 (IC50s = 480 and 181 nM, respectively); reverses cold-induced reductions in bladder capacity in anesthetized guinea pigs when administered as an i.v. infusion at 46.67 μg/kg per minute; decreases the core body temperature in rats at 100 and 300 mg/kg

Formal name: 3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-benzoic acid

Synonyms: 

Molecular weight: 428.5

CAS: 1398583-31-7

Purity: ≥98%

Formulation: A solid

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