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GSK 2193874
- Soluble in DMSO
- MF: C37H38BrF3N4O
- MW: 691.62
Description
GSK 2193874 is a potent, selective, and orally active TRPV4 channel blocker (IC50 values of 2 and 40 nM for rTRPV4 and hTRPV4, respectively). TRPV4 blockade with GSK 2193874 provided protection against the development of pulmonary edema and the resulting deficits in arterial oxygenation in heart failure models in vivo.
More Information
| Parent CAS No. | 1336960-13-4 |
|---|---|
| Chemical Name | 3-(1,4'-Bipiperidin-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-(3-(trifluoromethyl)phenyl)quinoline-4-carboxamide |
| SMILES | C1C=C2C(C(=O)NC3(CC3)C3C=CC=CC=3)=C(CN3CCC(N4CCCCC4)CC3)C(C3C=CC=C(C(F)(F)F)C=3)=NC2=CC=1Br |
| MFCD | N.A. |
| InChi | InChI=1S/C37H38BrF3N4O/c38-28-12-13-30-32(23-28)42-34(25-8-7-11-27(22-25)37(39,40)41)31(24-44-20-14-29(15-21-44)45-18-5-2-6-19-45)33(30)35(46)43-36(16-17-36)26-9-3-1-4-10-26/h1,3-4,7-13,22-23,29H,2,5-6,14-21,24H2,(H,43,46) |
| InChiKey | UIVOZBSCHXCGPS-UHFFFAOYSA-N |
| CID | 53464483 |
| Short Description | TRPV4 antagonist |
References
- KS Thorneloe 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.
- M Cheung 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.
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