Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 297 | 现货 | ||
2 mg | ¥ 438 | 现货 | ||
5 mg | ¥ 625 | 现货 | ||
10 mg | ¥ 1,120 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,870 | 现货 | ||
100 mg | ¥ 5,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 947 | 现货 |
产品描述 | GSK2193874 was identified as a selective, orally active TRPV4 blocker. |
靶点活性 | TRPV4 (human):40 nM (IC50), TRPV4 (rat):2 nM (IC50) |
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]. |
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]. |
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]. |
分子量 | 691.62 |
分子式 | C37H38BrF3N4O |
CAS No. | 1336960-13-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (144.59 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.4459 mL | 7.2294 mL | 14.4588 mL | 36.147 mL |
5 mM | 0.2892 mL | 1.4459 mL | 2.8918 mL | 7.2294 mL | |
10 mM | 0.1446 mL | 0.7229 mL | 1.4459 mL | 3.6147 mL | |
20 mM | 0.0723 mL | 0.3615 mL | 0.7229 mL | 1.8074 mL | |
50 mM | 0.0289 mL | 0.1446 mL | 0.2892 mL | 0.7229 mL | |
100 mM | 0.0145 mL | 0.0723 mL | 0.1446 mL | 0.3615 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GSK2193874 1336960-13-4 Membrane transporter/Ion channel TRP/TRPV Channel inhibit Transient receptor potential channels Inhibitor TRP Channel GSK-2193874 GSK 2193874 inhibitor