| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 1.8 nM (hTRPV4) and 1.6 nM (rTRPV4) | ||||||||||||
| Invitro | GSK2798745 inhibits TRPV4 agonist-induced impedance reduction in human umbilical vein endothelial cells (HUVECs)[3]. | ||||||||||||
| In Vivo | GSK2798745 inhibits TRPV4 agonist-mediated lung edema in rats in a dose-dependent manner[3]. Animal Model: | ||||||||||||
| Name | GSK2798745 | ||||||||||||
| CAS | 1419609-94-1 | ||||||||||||
| Formula | C25H28N6O3 | ||||||||||||
| Molar Mass | 460.53 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. |
GSK2798745
CAS: 1419609-94-1 F: C25H28N6O3 W: 460.53
GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocke
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