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SAR407899 hydrochloride
CAS No. 923262-96-8
SAR407899 hydrochloride ( —— )
产品货号. M27702 CAS No. 923262-96-8
SAR407899 盐酸盐是一种选择性、有效的 ATP 竞争性 ROCK 抑制剂，对 ROCK-2 的 IC50 为 135 nM，对人和大鼠 ROCK-2 的 Kis 分别为 36 nM 和 41 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥381 | 有现货 |
|
| 10MG | ￥583 | 有现货 |
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| 25MG | ￥1037 | 有现货 |
|
| 50MG | ￥1798 | 有现货 |
|
| 100MG | ￥2876 | 有现货 |
|
| 500MG | ￥6820 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称SAR407899 hydrochloride
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述SAR407899 盐酸盐是一种选择性、有效的 ATP 竞争性 ROCK 抑制剂，对 ROCK-2 的 IC50 为 135 nM，对人和大鼠 ROCK-2 的 Kis 分别为 36 nM 和 41 nM。
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产品描述SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.
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体外实验SAR407899 hydrochloride is a potent and ATP-competitive ROCK inhibitor, with Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 inhibits ROCK-2 better than ROCK-1, with IC50s of 102±19 nM and 276±26 nM, respectively, in the presence of 40 μM ATP. SAR407899 also less potently inhibits PKC-Δ and MSK-1, with IC50s of 5.4 and 3.1 μM, respectively. SAR407899 (0.1, 0.3, 1.0, and 3.0 μM) specifically inhibits the ROCK-mediated phosphorylation of MYPTT696 in HeLa cells stimulated with PHEN, and shows such effects at 1 μM and 10 μM in primary rat aortic smooth muscle cells. SAR407899 (3 μM) completely blocks thrombin-induced shrinkage of human umbilical vein endothelial cells (HUVECs) and stress fiber formation. SAR407899 concentration-dependently inhibits 5-bromodeoxyuridine incorporation into the cells with an IC50 of 5.0±1.3 μM. SAR407899 also effectively inhibits THP-1 migration with an IC50 of 2.5±1.0 μM. SAR407899 shows a potent vasorelaxant activity in a broad variety of isolated arteries taken from different vascular beds and species, with a range of IC50 values between 122 and 280 nM. SAR407899 dose-dependently relaxes the phenylephrine pre-contracted smooth muscle, with IC50s of 0.07 and 0.05 μM, respectively.
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体内实验SAR407899 (3 mg/kg, i.v.) inhibits ROCK-mediated phosphorylation of MYPTT696 in thoracic aorta of spontaneously hypertensive rats (SHRs). SAR407899 (0.01-0.30 mg/kg, i.v.) efficiently reduces pressor responses to vasoconstrictor agents in rats. SAR407899 (1, 3, 10, and 30 mg/kg, p.o.) dose dependently lowers blood pressure in hypertensive SHRs. SAR407899 (1-3 mg/kg, i.v. or 3, 10 mg/kg, p.o.) increases the length of the penis in healthy rabbits. SAR407899 (3-10 mg/kg, p.o.) also dose-dependently increases penile length in diabetic rabbits.
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同义词——
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通路Cell Cycle/DNA Damage
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靶点ROCK
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受体α1A-adrenergic receptor
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研究领域——
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适应症——
化学信息
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CAS Number923262-96-8
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分子量280.75
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分子式C14H17ClN2O2
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纯度>98% (HPLC)
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溶解度In Vitro:?H2O : 50 mg/mL (178.09 mM)
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SMILESCl.O=c1[nH]ccc2cc(OC3CCNCC3)ccc12
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Ford AP, et al. RS-17053 (N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-alpha, alpha-dimethyl-1H-indole-3-ethanamine hydrochloride), a selective alpha 1A-adrenoceptor antagonist, displays low affinity for functional alpha 1-adrenoceptors in human prostate: implications for adrenoceptor classification. Mol Pharmacol. 1996 Feb;49(2):209-15.
产品手册
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