| Identification | Back Directory | [Name]
URCMKDJBULWNAI-DQEYMECFSA-N | [CAS]
1419609-94-1 | [Synonyms]
GSK2798745
GSK-2798745,GSK2798745
URCMKDJBULWNAI-DQEYMECFSA-N
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]- | [Molecular Formula]
C25H28N6O3 | [MDL Number]
MFCD30489344 | [MOL File]
1419609-94-1.mol | [Molecular Weight]
460.53 |
| Chemical Properties | Back Directory | [Boiling point ]
682.1±65.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
12.73±0.29(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
GSK2798745 is a potent, selective, and 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 can be used in cardiac and respiratory diseases research[1][2][3]. | [in vivo]
GSK2798745 inhibits TRPV4 agonist-mediated lung edema in rats in a dose-dependent manner[3]. | Animal Model: | TRPV4-mediated lung edema in male Sprague-Dawley rats[3] | | Dosage: | 0, 16, 50, or 150 ng/kg | | Administration: | Intravenous injection; 0, 16, 50, or 150 ng/kg per minute; 60 min | | Result: | Inhibited the formation of pulmonary edema, with complete inhibition seen at the highest dose tested where the basal lung wet weight to body weight ratio was held to control levels (LW/BW=4.21). |
| [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. DOI:10.1007/s40256-018-00320-6
[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. DOI:10.1021/acsmedchemlett.9b00274
[3] Xiaoping Xu, et al. Identification of a Human Whole Blood-Based Endothelial Cell Impedance Assay for Assessing Clinical Transient Receptor Potential Vanilloid 4 Target Engagement Ex Vivo. J Pharmacol Exp Ther. 2021 Mar;376(3):436-443. DOI:10.1124/jpet.120.000307 |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
Biorbyt Ltd.
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| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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