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SAR407899 是一种选择性的 ATP 竞争性ROCK 抑制剂,对ROCK-2的IC50值为 135 nM,对人和大鼠ROCK-2的Ki 值分别为 36 和 41 nM。它是 Rho 激酶抑制剂,有效抑制 endothelin-1 诱导的肾阻力动脉收缩。
SAR407899 是一种选择性的 ATP 竞争性ROCK 抑制剂,对ROCK-2的IC50值为 135 nM,对人和大鼠ROCK-2的Ki 值分别为 36 和 41 nM。它是 Rho 激酶抑制剂,有效抑制 endothelin-1 诱导的肾阻力动脉收缩。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 218 | 现货 | |
2 mg | ¥ 297 | 现货 | |
5 mg | ¥ 496 | 现货 | |
10 mg | ¥ 745 | 现货 | |
25 mg | ¥ 1,380 | 现货 | |
50 mg | ¥ 2,230 | 现货 | |
100 mg | ¥ 3,560 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 546 | 现货 |
产品描述 | SAR407899 is Rho kinase inhibitor potently inhibits endothelin-1-induced constriction of renal resistance arteries. |
靶点活性 | ROCK1:276 nM (IC50), ROCK2:102 nM (IC50) |
体内活性 | 在体内,SAR407899 剂量依赖性地诱导兔子阴茎勃起,与 sildenafil[1] 相比,其效力更大,作用时间更长。 |
动物实验 | Compared the effects of SAR407899, the Rho-kinase inhibitor Y-27632 and the PDE5 inhibitor sildenafil for their ability to relax corpus cavernosum strips contracted with phenylephrine in healthy and diabetic animals. Strips were obtained from WKY, spontaneous hypertensive (SHR), control CD, and diabetic CD rats, humans, control and diabetic rabbits. Diabetes was induced by streptozotocin or alloxan injection. In vivo penile erection (length) induced by drugs was measured in conscious rabbits[1]. |
分子量 | 244.29 |
分子式 | C14H16N2O2 |
CAS No. | 923359-38-0 |
Smiles | O=c1[nH]ccc2cc(OC3CCNCC3)ccc12 |
密度 | 1.193 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 6 mg/mL (24.56 mM) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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