GSK2798745 |
Catalog No.GC39387 |
GSK2798745는 hTRPV4 및 rTRPV4에 대해 각각 1.8nM 및 1.6nM의 IC50를 가진 강력하고 선택적이며 경구 흡수성 transient receptor potential vanilloid 4 (TRPV4) 이온 채널 차단제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1419609-94-1
Sample solution is provided at 25 µL, 10mM.
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].
[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.
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