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GSK2798745

Katalog-Nr.GC39387

GSK2798745 ist ein potenter, selektiver und oral aktiver Blocker des transienten Rezeptorpotentials Vanilloid 4 (TRPV4)-Ionenkanals mit IC50-Werten von 1,8 bzw. 1,6 nM für hTRPV4 und rTRPV4.

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GSK2798745 Chemische Struktur

Cas No.: 1419609-94-1

Größe Preis Lagerbestand Menge
10mM (in 1mL DMSO)
688,00 $
Auf Lager
1mg
250,00 $
Auf Lager
5mg
626,00 $
Auf Lager

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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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