GSK2798745

Names

[ CAS No. ]:
1419609-94-1

[ Name ]:
GSK2798745

[Synonym ]:
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]-

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
682.1±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₅H₂₈N₆O₃

[ Molecular Weight ]:
460.528

[ Flash Point ]:
366.3±34.3 °C

[ Exact Mass ]:
460.222290

[ LogP ]:
1.76

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.680

[ Storage condition ]:
2-8°C

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.