1336960-13-4 Usage
Uses
Different sources of media describe the Uses of 1336960-13-4 differently. You can refer to the following data:
1. GSK 2193874 is an orally active, potent and selective TRPV4 antagonist.
2. GSK2193874 has been used as a transient receptor potential vanilloid 4 (TRPV4) antagonist:to study its effects on GSK101-induced colon contractions in miceto study its effects on murine compact bone-derived osteoblasts(CB-OB)to study its effects on lung injury post-lipopolysaccharide (LPS) in mice
Biochem/physiol Actions
GSK2193874 is a very potent, specific antagonist of TRPV4 ion channels (IC50 = 50 nM). Lung edema caused by high pulmonary venous pressure (PVP) is driven by TRPV4 activity. GSK2193874 blocks TRPV4-mediated calcium influx in cells expressing native and recombinant TRPV4, and inhibits vascular permeability and lung edema in isolated rodent and canine lungs subjected to high PVP. The compound also resolves pulmonary edema in murine myocardial infarction model.
Check Digit Verification of cas no
The CAS Registry Mumber 1336960-13-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,3,6,9,6 and 0 respectively; the second part has 2 digits, 1 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1336960-13:
(9*1)+(8*3)+(7*3)+(6*6)+(5*9)+(4*6)+(3*0)+(2*1)+(1*3)=164
164 % 10 = 4
So 1336960-13-4 is a valid CAS Registry Number.
1336960-13-4Relevant articles and documents
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4
Cheung, Mui,Bao, Weike,Behm, David J.,Brooks, Carl A.,Bury, Michael J.,Dowdell, Sarah E.,Eidam, Hilary S.,Fox, Ryan M.,Goodman, Krista B.,Holt, Dennis A.,Lee, Dennis,Roethke, Theresa J.,Willette, Robert N.,Xu, Xiaoping,Ye, Guosen,Thorneloe, Kevin S.
, p. 549 - 554 (2017/05/19)
Transient Receptor Potential Vanilloid 4 (TRPV4) is a member of the Transient Receptor Potential (TRP) superfamily of cation channels. TRPV4 is expressed in the vascular endothelium in the lung and regulates the integrity of the alveolar septal barrier. Increased pulmonary vascular pressure evokes TRPV4-dependent pulmonary edema, and therefore, inhibition of TRPV4 represents a novel approach for the treatment of pulmonary edema associated with conditions such as congestive heart failure. Herein we report the discovery of an orally active, potent, and selective TRPV4 blocker, 3-(1,4′-bipiperidin-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide (GSK2193874, 28) after addressing an unexpected off-target cardiovascular liability observed from in vivo studies. GSK2193874 is a selective tool for elucidating TRPV4 biology both in vitro and in vivo.
