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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-GSK2193874
GSK2193874

Chemical Structure : GSK2193874

CAS No.: 1336960-13-4

GSK2193874 (GSK 2193874, GSK-2193874)

货号: PC-60294Not For Human Use, Lab Use Only.

GSK2193874 (GSK 2193874) is an orally active, potent, and selective blocker of TRPV4 channel with IC50 of 40 nM and 2 nM for hTRPV4 and rTRPV4, respectively.

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25 mg ¥2180 In stock
50 mg ¥3680 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK2193874 (GSK 2193874) is an orally active, potent, and selective blocker of TRPV4 channel with IC50 of 40 nM and 2 nM for hTRPV4 and rTRPV4, respectively.
GSK2193874 shows high selectivity against TRPV1, TRPA1, TRPC3, TRPC6, TRPM8 (IC50>25 uM).
GSK2193874 is the first-in-class orally bioavailable TRPV4 inhibitor which demonstrates ability to improve pulmonary functions in a number of heart failure models.

物理化学性质&存储条件

分子量 691.62
分子式 C37H38BrF3N4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(1,4'-bipiperidin-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide

参考文献

1. Cheung M, et al. ACS Med Chem Lett. 2017 Mar 20;8(5):549-554.

2. Buday T, et al. Respir Physiol Neurobiol. 2017 Feb;236:1-4.

3. Thorneloe KS, et al. Sci Transl Med. 2012 Nov 7;4(159):159ra148.

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