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PENTOSTATIN| 货号： | R11033 |
| CAS号： | 923359-38-0 |
| 供应商： | 上海芮晖化工 |
| 数量： | 1g |
| 英文名： | SAR407899 |
| 保质期： | 两年 |
| 保存条件： | 冷冻 |
| 规格： | 5mg/10mg/50mg |
SAR407899是ROCK激酶高效选择性抑制剂，对人源和属源ROCK的Ki值分别为36nM和41nM。
SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.
IC50 value: 36 nM/41 nM(Ki, human/Rat ROCK)
Target: ROCK inhibitor
in vitro: SAR407899 is highly selective in panel of 117 receptor and enzyme targets. SAR407899 is ≈8-fold more active than fasudil. In vitro, SAR407899 demonstrated concentration-dependent inhibition of Rho-kinase–mediated phosphorylation of myosin phosphatase, thrombin-induced stress fiber formation, platelet-derived growth factor–induced proliferation, and monocyte chemotactic protein-1–stimulated chemotaxis. SAR407899 potently (mean IC50 values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds [1]. SAR407899 dose-dependently relaxed the pre-contracted corpora cavernosa in all species, with similar potency and efficacy in healthy vs diabetic rats, WKY vs SHR rats, healthy vs diabetic rabbits (IC(50) range from 0.05 to 0.29 μM, Emax range 89 to 97%) [3].
in vivo: Over the dose range 3 to 30 mg/kg PO, SAR407899 lowered blood pressure in a variety of rodent models of arterial hypertension [1]. SAR407899 was more effective than Y27632 in reducing ET-1-induced vasoconstriction in ZDF rat renal resistance arteries. Maximum ET-1-induced vasoconstriction in SAR407899-treated and Y27632-treated human renal resistance arteries was 23±5 and 48±6% of control values, respectively.
