S86881 |
ROCK-IN-2 ( Azaindole 1; TC-S 7001) |
源叶(MedMol) | ≥98%(HPLC) |
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- 产品描述: BAY-549 (Azaindole 1) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively
- 靶点: ROCK-1:0.6 nM (IC50);ROCK-2:1.1 nM (IC50);TRK:252 nM (IC50);FLT3:303 nM (IC50);ROCK
- 体内研究:
BAY-549 (Azaindole 1) (0.03, 0.1, 0.3 mg/kg, i.v.) results in a dose-dependent and long-lasting decrease in blood pressure in anaesthetized normotensive rats. BAY-549 (3 and 10 mg/kg, p.o.) decreases blood pressure dose-dependently and persistently both in normotensive and hypertensive rats, and shows such effects even at 1 mg/kg in hypertensive rats. BAY-549 (0.1 and 0.3 mg/kg, i.v. bolus injections) causes decreased mean arterial blood pressure in a dose-related manner and only leads to a moderate and dose-independent increase in heart rate of anaesthetized dogs
- 参考文献:
1. Kast R, et al. Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br J Pharmacol. 2007 Dec;152(7):1070-80. Epub 2007 Oct 15.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.483 ml 12.414 ml 24.827 ml 5 mM 0.497 ml 2.483 ml 4.965 ml 10 mM 0.248 ml 1.241 ml 2.483 ml 50 mM 0.05 ml 0.248 ml 0.497 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)