规格

价格

库存

数量

1 mg

¥ 255

现货

2 mg

¥ 375

现货

5 mg

¥ 535

现货

10 mg

¥ 950

现货

25 mg

¥ 1,690

现货

50 mg

¥ 3,300

现货

100 mg

¥ 4,800

现货

1 mL x 10 mM (in DMSO)

¥ 812

现货

生物活性

产品描述	GSK2193874 was identified as a selective, orally active TRPV4 blocker.
靶点活性	TRPV4 (rat):2 nM (IC50), TRPV4 (human):40 nM (IC50)
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]。
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]。
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].

化学信息

分子量	691.62
分子式	C₃₇H₃₈BrF₃N₄O
CAS No.	1336960-13-4
Smiles	FC(F)(F)c1cccc(c1)-c1nc2cc(Br)ccc2c(C(=O)NC2(CC2)c2ccccc2)c1CN1CCC(CC1)N1CCCCC1
密度	1.43 g/cm3 (Predicted)

储存&溶解度

存储

溶解度信息

DMSO: 81.67 mg/mL (118.09 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (5.78 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.4459 mL	7.2294 mL	14.4588 mL	72.2940 mL
5 mM	0.2892 mL	1.4459 mL	2.8918 mL	14.4588 mL
10 mM	0.1446 mL	0.7229 mL	1.4459 mL	7.2294 mL
20 mM	0.0723 mL	0.3615 mL	0.7229 mL	3.6147 mL
50 mM	0.0289 mL	0.1446 mL	0.2892 mL	1.4459 mL
100 mM	0.0145 mL	0.0723 mL	0.1446 mL	0.7229 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

GSK2193874

GSK2193874

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词

GSK2193874

GSK2193874

GSK2193874 相关产品

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词