General description
A pyrrolocarboxamide compound that potently antagonizes TRP (transient receptor potential) family cation channel TRPV4 activity (IC50 = 17, 48, and 133 nM, respectively, against mouse, human, or rat TRPV4 in whole cell voltage-gated current measurement) in a reversible manner, displaying much reduced potency against human ERG and TRPM8 (IC50 = 368 and 780 nM, respectively) and little or no activity toward hKv1.3, hTRPA1, hTRPC5, hTRPV1/2/3/6, mTRPM7, mTRPV2, or rKv1.2. HC-067047 is efficacious (10 mg/kg via i.p.) in reducing micturition (urination) frequency and increasing voided urine volume of mice and rats suffering from CPA- (Cat. No. 239785) induced cystitis in vivo.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Everaerts, W., et al. 2010. Proc. Natl. Acad. Sci. USA107, 19084.
Packaging
Packaged under inert gas
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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