GSK2193874

GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50s of 2 nM and 40 nM for rTRPV4 and hTRPV4[1].

Product Specifications

CAS Number

[1336960-13-4]

UNSPSC

12352005

Hazard Statement

H301, H315, H319, H335

Target

TRP Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/GSK2193874.html

Purity

99.91

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=C(CN2CCC(N3CCCCC3)CC2)C(C4=CC=CC(C(F)(F)F)=C4)=NC5=CC(Br)=CC=C15)NC6(C7=CC=CC=C7)CC6

Molecular Formula

C37H38BrF3N4O

Molecular Weight

691.62

Precautions

H301, H315, H319, H335

References & Citations

[1]Cheung M, et al. Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4. ACS Med Chem Lett. 2017 Mar 20;8 (5) :549-554.|[2]Thorneloe KS, et al. An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci Transl Med. 2012 Nov 7;4 (159) :159ra148.