1419609-94-1

1419609-94-1 structure

Name: GSK2798745
Chemical Name: 1-({(5S,7S)-3-[5-(2-Hydroxy-2-propanyl)-2-pyrazinyl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]dec-7-yl}methyl)-1H-benzimidazole-6-carbonitrile
CAS Number: 1419609-94-1
Molecular Formula: C₂₅H₂₈N₆O₃
Molecular Weight: 460.528
Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
Create Date: 2018-07-03 16:44:45
Modify Date: 2024-01-03 06:31:56
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].

Name	1-({(5S,7S)-3-[5-(2-Hydroxy-2-propanyl)-2-pyrazinyl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]dec-7-yl}methyl)-1H-benzimidazole-6-carbonitrile
Synonyms	1-({(5S,7S)-3-[5-(2-Hydroxy-2-propanyl)-2-pyrazinyl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]dec-7-yl}methyl)-1H-benzimidazole-6-carbonitrile 1H-Benzimidazole-6-carbonitrile, 1-[[(5S,7S)-3-[5-(1-hydroxy-1-methylethyl)-2-pyrazinyl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]dec-7-yl]methyl]-

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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel Research Areas >> Cardiovascular Disease
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.