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GSK2798745

  Cat. No.:  DC26197   Featured
Chemical Structure
1419609-94-1
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More than 5000 active chemicals with high quality for research!
Field of application
GSK2798745 is an inhibitor of the transient receptor potential vanilloid 4 (TRPV4) with IC50 of 1.8nM.
Cas No.: 1419609-94-1
Chemical Name: GSK2798745
Synonyms: 1-(((5S,7S)-3-(5-(2-hydroxypropan-2-yl)pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl)methyl)-1H-benzo[d]imidazole-6-carbonitrile;GSK2798745;63FJ7LF55O;URCMKDJBULWNAI-DQEYMECFSA-N;3-[[(5S,7S)-3-[5-(2-Hydroxypropan-2-yl)pyrazin-2-yl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl];3-[[(5S,7S)-3-[5-(2-hydroxypropan-2-yl)pyrazin-2-yl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl]methyl]benzimidazole-5-carbonitrile;BDBM50502640;AT16701;1-(((5S,7S)-3-(5-(2-Hydroxypropan-2-yl)pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-azaspiro(4.5)decan-7-yl)methyl)-1hbenzo(d)imidazole-6-carbonitrile;1-(((5S,7S)-3-(5-(2-hydroxypropan-2-yl)pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-az;Unii-63FJ7LF55O
SMILES: O1C(N(C2C=NC(C(C)(C)O)=CN=2)C[C@]21CCC[C@](C)(CN1C=NC3C=CC(C#N)=CC1=3)C2)=O
Formula: C25H28N6O3
M.Wt: 460.528224945068
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
Description: GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 is used in research for the treatment of pulmonary edema associated with congestive heart failure[1][2].
Target: IC50: 1.8 nM (hTRPV4) and 1.6 nM (rTRPV4)[2]
References: [1]. Goyal N, et al. Clinical Pharmacokinetics, Safety, and Tolerability of a Novel, First-in-Class TRPV4 Ion Channel Inhibitor, GSK2798745, in Healthy and Heart Failure Subjects. Am J Cardiovasc Drugs. 2019 Jun;19(3):335-342. [2]. Brooks CA, et al. Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4). ACS Med Chem Lett. 2019 Jul 15;10(8):1228-1233.
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