GSK-1016790A, TRPV4 channel activator

Product Details

Formal Name: (N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide

Molecular Formula: C₂₈H₃₂Cl₂N₄O₆S₂

Formula Weight: 655.62

CAS Number: 942206-85-1

Purity: >98%

Formulation: powder

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

Storage: -20°C

Stability: ≥ 2 years.

Applications

TRPV4 channel activator

Functions

A novel and potent TRPV4 channel agonist. GSK1016790A induced Ca²⁺ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300-fold more potent than 4α-PDD and is a valuable tool for investigating the role of TRPV4 in physiological processes.

Application Procedures

First dissolved in DMSO (up to 10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 2 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)