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GSK-2193874

Chemical Structure : GSK-2193874

CAS No.: 1336960-13-4

GSK-2193874 (GSK 2193874;GSK2193874)

Catalog No.: PC-60294Not For Human Use, Lab Use Only.

GSK-2193874 (GSK2193874) is an orally active, potent, and selective blocker of TRPV4 channel with IC50 of 40 nM and 2 nM for hTRPV4 and rTRPV4, respectively.

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Biological Activity

GSK-2193874 (GSK2193874) is an orally active, potent, and selective blocker of TRPV4 channel with IC50 of 40 nM and 2 nM for hTRPV4 and rTRPV4, respectively; shows high selectivity against TRPV1, TRPA1, TRPC3, TRPC6, TRPM8 (IC50>25 uM); the first-in-class orally bioavailable TRPV4 inhibitor which demonstrates ability to improve pulmonary functions in a number of heart failure models.

Physicochemical Properties

M.Wt 691.62
Formula C37H38BrF3N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(1,4'-bipiperidin-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide

References

1. Cheung M, et al. ACS Med Chem Lett. 2017 Mar 20;8(5):549-554.

2. Buday T, et al. Respir Physiol Neurobiol. 2017 Feb;236:1-4.

3. Thorneloe KS, et al. Sci Transl Med. 2012 Nov 7;4(159):159ra148.

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