GSK2798745

Modify Date: 2025-08-23 21:28:08

GSK2798745 Structure
GSK2798745 structure
Common Name GSK2798745
CAS Number 1419609-94-1 Molecular Weight 460.528
Density 1.4±0.1 g/cm3 Boiling Point 682.1±65.0 °C at 760 mmHg
Molecular Formula C25H28N6O3 Melting Point N/A
MSDS N/A Flash Point 366.3±34.3 °C

 Use of GSK2798745


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].

 Names

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
Synonym More Synonyms

 GSK2798745 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
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

 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]-
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