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- 文献和实验
- 技术资料
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Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：1-2天
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MedChemExpress LLC
- CAS号：
923359-38-0
- 规格：
10 mM * 1 mL/2 mg/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥806.0 |
|---|---|---|---|
| 规格： | 2 mg | 产品价格： | ￥600.0 |
| 规格： | 5 mg | 产品价格： | ￥990.0 |
| 规格： | 10 mg | 产品价格： | ￥1700.0 |
| 规格： | 50 mg | 产品价格： | ￥5900.0 |
| 规格： | 100 mg | 产品价格： | ￥9900.0 |
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SAR407899
CAS No. : 923359-38-0
MCE 国际站：SAR407899
产品活性：SAR407899 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 Ki 值分别为 36 nM 和 41 nM。SAR407899对迁移体的形成有稳定的抑制作用。
研究领域：Cell Cycle/DNA Damage | Stem Cell/Wnt | Cytoskeleton | TGF-beta/Smad
作用靶点：ROCK
In Vitro: SAR407899 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.
In Vivo: 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.
相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | TGF-beta/Smad Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Reprogramming Compound Library | Anti-diabetic Compound Library | Anti-COVID-19 Compound Library | Cytoskeleton Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Serine/Threonine Kinase Inhibitor Library | Y-27632 dihydrochloride | Chroman 1 | Belumosudil | Fasudil Hydrochloride | Thiazovivin | Narciclasine | Afuresertib | H-1152 dihydrochloride | GSK269962A | GSK429286A | Ripasudil | CCG-222740 | AT13148 | Y-33075 | LX7101 | HA-100 | GSK180736A | RKI-1447 | ROCK inhibitor-2 | SR-3677 | Pentanoic acid | Verosudil | BDP5290 | CRT0066854 | Hydroxyfasudil | SAR407899 hydrochloride
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