616521

TRPV4 Antagonist II, HC-067047

The TRPV4 Antagonist II, HC-067047 controls the biological activity of TRPV4.

• Synonym(s): TRPV4 Antagonist II, HC-067047, 2-Methyl-1-(3-morpholinopropyl)-5-phenyl-N-(3-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide, Transient Receptor Potential Vanilloid-4 Antagonist II, HC067047, HC067047, 2-Methyl-1-(3-morpholinopropyl)-5-phenyl-N-(3-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide, Transient Receptor Potential Vanilloid-4 Antagonist II
• Empirical Formula (Hill Notation): C₂₆H₂₈F₃N₃O₂
• CAS Number: 883031-03-6
• Molecular Weight: 471.51
• MDL number: MFCD01571257
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• 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

Description

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 hK_v1.3, hTRPA1, hTRPC5, hTRPV1/2/3/6, mTRPM7, mTRPV2, or rK_v1.2. 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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable