GSK1016790A

GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca2+ influx and elevate intracellular Ca2+ in HEK cells[1][2].

Product Specifications

CAS Number

[942206-85-1]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Calcium Channel; TRP Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/GSK1016790A.html

Purity

99.93

Solubility

DMSO : ≥ 33 mg/mL|Methanol : 50 mg/mL (ultrasonic)

Smiles

O=C(C1=CC2=CC=CC=C2S1)N[C@H](C(N3CCN(C([C@@H](NS(=O)(C4=CC=C(Cl)C=C4Cl)=O)CO)=O)CC3)=O)CC(C)C

Molecular Formula

C28H32Cl2N4O6S2

Molecular Weight

655.61

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Kevin S Thorneloe, et al. N- ((1S) -1-{[4- ((2S) -2-{[ (2,4-dichlorophenyl) sulfonyl]amino}-3-hydroxypropanoyl) -1-piperazinyl]carbonyl}-3-methylbutyl) -1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326 (2) :432-42.|[2]J Fichna, et al. Transient receptor potential vanilloid 4 inhibits mouse colonic motility by activating NO-dependent enteric neurotransmission. J Mol Med (Berl) . 2015 Dec;93 (12) :1297-309.