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GSK2193874

GSK2193874 是口服有效的TRPV4选择性拮抗剂，作用于rTRPV4和hTRPV4的IC50分别为 2 nM 和 40 nM。

CAS号

1336960-13-4

分子式

C37H38BrF3N4O

主要靶点

TRP/TRPV Channel

仅限科研使用

Cat No : CM06802

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Synonyms

验证数据展示

  • CAS No.: 1336960-13-4

    GSK2193874
    CAS#: 1336960-13-4

产品信息

GSK2193874 was identified as a selective, orally active TRPV4 blocker.

CAS号 1336960-13-4
分子式 C37H38BrF3N4O
主要靶点 TRP/TRPV Channel
主要通路 离子通道
分子量 691.6
纯度 98.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

rTRPV4:2 nM (IC50)|hTRPV4:40 nM (IC50)

体内活性

In isolated rodent and canine lungs, TRPV4 blockade prevented the increased vascular permeability and resultant pulmonary edema associated with elevated PVP. ?In both acute and chronic HF models, GSK2193874 pretreatment inhibited the formation of pulmonary edema and enhanced arterial oxygenation[2].

体外活性

GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents[1,2].

溶解度

DMSO:100 mg/mL (144.59 mM)

动物实验

Adult male Sprague-Dawley rats (n = 7 to 8 per group) were treated with vehicle (6% Cavitron) or GSK2193874 (30 mg/kg/day) via oral gavage for at least 4 days before osmotic challenges.?Rats underwent acute and chronic hyper- and hypo-osmotic challenges.Sprague-Dawley (control, n = 18) and spontaneously hypertensive rats (n = 11) were implanted with Data Sciences International (DSI) radiotelemetry transmitters.?Rats were dosed with GSK2193874, and data were captured with DSI receivers and analyzed with Microsoft Excel[2].

参考文献

1.Cheung M , Bao W , Behm D J , et al. Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4[J]. ACS Medicinal Chemistry Letters, 2017:acsmedchemlett.7b00094.
2.Thorneloe K S , Cheung M , Bao W , et al. An Orally Active TRPV4 Channel Blocker Prevents and Resolves Pulmonary Edema Induced by Heart Failure[J]. Science Translational Medicine, 2012, 4(159):159ra148-159ra148.

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