GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 ( TRPV4 ) ion channel blocker with IC 50 s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases research In Vitro GSK2798745 inhibits TRPV4 agonist-induced impedance reduction in human umbilical vein endothelial cells (HUVECs). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GSK2798745 inhibits TRPV4 agonist-mediated lung edema in rats in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: TRPV4-mediated lung edema in male Sprague-Dawley ratsDosage: 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). Form:Solid IC50& Target:IC50: 1.8 nM (hTRPV4) and 1.6 nM (rTRPV4)
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GSK2798745
CAS number：1419609-94-1 molecular formula：C25H28N6O3
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| Chinese alias | - | ||
| English alias | 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 | URCMKDJBULWNAI-DQEYMECFSA-N | GSK2798745 | GSK-2798745 | 1-(((5S,7S)-3-(5-(2-hydroxypropan-2-yl)pyrazin-2-yl)- | ||
| CAS number | 1419609-94-1 | molecular formula | C25H28N6O3 |
| molecular weight | 460.53 g/mol | Exact mass | ≥99% |
| PSA | 117.000 Ų | logp | 2 |
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