HC-067047, TRPV4 blocker

Product Details

Formal Name: 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide

Molecular Formula: C₂₆H₂₈F₃N₃O₂

Formula Weight: 471.51

CAS Number: 883031-03-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 10 mg/ml).

Storage: -20°C

Stability: ≥ 2 years.

Applications

TRPV4 blocker

Functions

Potent reversible and selective TRPV4 antagonist. Active at mouse, human and rat TRPV4,  IC50 = 17, 48 and 133 nM respectively. Also inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM). Selective for TRPV4 over TRPV1, TRPV2, TRPV3 and TRPM8 channels. Increases functional bladder capacity and reduces micturition frequency in mice and rats with cystitis. Inhibits brain edema in middle cerebral artery occlusion mice. Induces an increase in core body temperature accompanied by increased oxygen consumption in Wistar rats. Active in vivo.

Application Procedures

First dissolved in DMSO (up to 50 mg/ml) or in Ethanol (up to 10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)