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GSK2193874

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

inhibit|GSK2193874|GSK-2193874|GSK 2193874|Inhibitor|TRPV4|TRPV Channel|TRPChannel|TRPVChannel|Transient receptor potential channels|TRP Channel

验证数据展示

  • CAS No.: 1336960-13-4

    GSK2193874
    CAS#: 1336960-13-4

产品信息

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 691.62
纯度 98.79%， 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 | Shipping with blue ice.
别名 inhibit|GSK2193874|GSK-2193874|GSK 2193874|Inhibitor|TRPV4|TRPV Channel|TRPChannel|TRPVChannel|Transient receptor potential channels|TRP Channel

靶点活性

TRPV4 (rat):2 nM (IC50)|TRPV4 (human):40 nM (IC50)

体内活性

在分离的啮齿类和犬类肺部中，TRPV4阻断能够防止与升高的PVP相关联的增加的血管通透性和由此导致的肺水肿。在急性和慢性HF模型中，GSK2193874的预处理抑制了肺水肿的形成并提高了动脉氧合[2]。

体外活性

GSK2193874被确定为一种选择性、口服活性的TRPV4阻断剂，能够抑制通过重组TRPV4通道以及天然内皮TRPV4电流的Ca(2+)流入[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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