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SAR407899 hydrochloride

CAS No. : 923262-96-8

MCE 站：SAR407899 hydrochloride

产品活性：SAR407899 hydrochloride 是一种选择性的，有效的，ATP 竞争性的 ROCK 抑制剂，对 ROCK-2 的 IC₅₀ 值为 135 nM，对人和大鼠 ROCK-2 的 K_i 值分别为 36 nM 和 41 nM。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  Cytoskeleton  |  TGF-beta/Smad

作用靶点：ROCK

In Vitro: SAR407899 hydrochloride is a potent and ATP-competitive ROCK inhibitor, with K_is 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 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 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.

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.

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