GSK2193874

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Chemical Structure| 1336960-13-4 同义名 : -
CAS号 : 1336960-13-4
货号 : A892019
分子式 : C37H38BrF3N4O
纯度 : 99%+
分子量 : 691.62
MDL号 : MFCD28009510
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 GSK2193874 is an orally administered, highly potent, and selective antagonist of TRPV4, demonstrating IC50 values of 2 nM for rTRPV4 and 40 nM for hTRPV4. When tested against various TRP channels, GSK2193874 shows selectivity, with no significant activity against TRPV1, TRPA1, TRPC3, TRPC6, and TRPM8, all having IC50 values greater than 25 μM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.45mL

0.29mL

0.14mL

7.23mL

1.45mL

0.72mL

14.46mL

2.89mL

1.45mL
参考文献

[1]Cheung M, Bao W, et al. Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4. ACS Med Chem Lett. 2017 Mar 20;8(5):549-554.

[2]Thorneloe KS, Cheung M, et al. An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci Transl Med. 2012 Nov 7;4(159):159ra148.

[3]Mori A, Takeda K, et al. Activation of transient receptor potential vanilloid 4 channels dilates rat retinal arterioles through nitric oxide- and BKCa channel-dependent mechanisms in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2020 Jan;393(1):35-41.

[4]Yao L, Chen S, et al. Transient Receptor Potential Ion Channels Mediate Adherens Junctions Dysfunction in a Toluene Diisocyanate-Induced Murine Asthma Model. Toxicol Sci. 2019 Mar 1;168(1):160-170.