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.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Everaerts, W., et al. 2010. Proc. Natl. Acad. Sci. USA107, 19084.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 471.51. Empirical Formula: C26H28F3N3O2. Quality Level: 100. Assay: ≥. 98% (HPLC). form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 50 . mg/mL, clear, colorless. shipped in: ambient. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 616521-10MG