计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC 50 of 135 nM for ROCK-2 , and K i s of 36 nM and 41 nM for human and rat ROCK-2 , respectively.
In Vitro
SAR407899 hydrochloride is a potent and ATP-competitive ROCK inhibitor, with K i s of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 inhibits ROCK-2 better than ROCK-1, with IC 50 s 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 IC 50 s 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 MYPT T696 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 IC 50 of 5.0±1.3 μM. SAR407899 also effectively inhibits THP-1 migration with an IC 50 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 IC 50 values between 122 and 280 nM. SAR407899 dose-dependently relaxes the phenylephrine pre-contracted smooth muscle, with IC 50 s of 0.07 and 0.05 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SAR407899 (3 mg/kg, i.v.) inhibits ROCK-mediated phosphorylation of MYPT T696 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
Rabbits are treated either intravenously (i.v., in an ear vein) with increasing doses of SAR407899 (0.3, 1, 3, 10 mg/kg) or orally with SAR407899 (1, 3, 10, 30 mg/kg) or sildenafil (2 or 6 mg/kg). Each animal is used several times for different doses and different agents, always with a week's washout. The length (mm) of uncovered penile mucosa (penile erection parameter) is measured at different time-points, using a sliding digital caliper. The results are expressed as mean ± SEM penile length of 3-5 rabbits . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:ROCK-2 102 nM (IC 50 ) ROCK-1 276 nM (IC 50 )
规格
别名
SAR407899盐酸盐
规格或纯度
10mM in DMSO
英文名称
SAR407899 hydrochloride
生化机理
SAR407899 盐酸盐是一种选择性、强效和 ATP 竞争性 ROCK 抑制剂，对 ROCK-2 的 IC 50 为 135 nM，对人类和大鼠 ROCK-2 的 K i s 分别为 36 nM 和 41 nM。
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
Rho- 相关蛋白激酶抑制剂
名称和识别符
技术文档
高级数据
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溶液计算器
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