Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK), which can penetrate the central nervous system (CNS). It exhibits a high affinity for ROCK2 with an inhibition constant (IC50) of 3 nM. This compound is of potential interest for further investigations in the field of Huntington's disease research [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,540 | 5日内发货 | ||
5 mg | ¥ 2,610 | 5日内发货 | ||
25 mg | ¥ 9,160 | 6-8周 | ||
50 mg | ¥ 11,900 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,730 | 5日内发货 |
产品描述 | Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK), which can penetrate the central nervous system (CNS). It exhibits a high affinity for ROCK2 with an inhibition constant (IC50) of 3 nM. This compound is of potential interest for further investigations in the field of Huntington's disease research [1]. |
体外活性 | Rho-Kinase-IN-2 (0-10 mM, 1 hour) treatment shows an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation [1]. Western Blot Analysis [1] Cell Line: A7r5 and PANC1 cells Concentration: 0-10 mM Incubation Time: 1 hour Result: Showed concentration-dependent effects, leading to an increase in AKT phosphorylation (EC 50 =28 nM) and a decrease in MYPT1 phosphorylation (IC 50 =14 nM). |
体内活性 | Rho-Kinase-IN-2 (Oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h) treatment shows dose- and time-dependent ROCK1 and ROCK2 target engagement [1]. Rho-Kinase-IN-2 (Oral adiministration; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment shows excellent tolerability assessment [1]. Rho-Kinase-IN-2 (Oral adiministration; 1-20 mg/kg; once) treatment shows a direct dose- and time-dependent relationship between brain exposure and MYPT1 phosphorylation status [1]. Rho-Kinase-IN-2 (Oral adiministration; 10 or 20 mg/kg; once) treatment decreases in the mean arterial, systolic, diastolic blood pressure, and heart rate [1]. Rho-Kinase-IN-2 (Oral adiministration; 10 mg/kg; twice a day; 90 days) treatment leads to lower-than-expected brain concentrations [1]. Animal Model: Male C57BL/6 mice [1] Dosage: 10 mg/kg Administration: Oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h Result: Observed dose- and time-dependent ROCK1 and ROCK2 TE, with a free brain KiNativ ROCK1 and ROCK2 IC 50 =~6 nM. Animal Model: 3 4 months old heterozygote Q175DN KI and wild-type littermate mice [1] Dosage: 10 or 20 mg/kg Administration: Oral adiministration; 10 or 20 mg/kg; once a day or twice a day; 2 weeks Result: Scored neurological index normally at all doses although a slight loss in bodyweight (~2%) in the 20 mg/kg treatment group. Animal Model: Heterozygote HTT zQ175DN knock-in mice [1] Dosage: 1-20 mg/kg Administration: Oral adiministration; 1-20 mg/kg; once Result: Remained over MYPT1 IC 50 for over 2 h of the free brain at 10 mg/kg, and observed the dose- and time-dependent inhibition of MYPT1 phosphorylation in the striatum following acute in vivo dosing. Animal Model: CD1 mice [1] Dosage: 10 and 20 mg/kg Administration: Oral adiministration; 10 or 20 mg/kg; once Result: Observed the decreases in the mean arterial (maximum change of 61.0 ± 8.5 mmHg from baseline), systolic (maximum change of 59.5 ± 8.4 mmHg from baseline), diastolic blood pressure (maximum change of 56.4 ± 9.0 mmHg from baseline), and heart rate (maximum change from predose of 107 bpm) when compared to the control group from ~0.5 to 2 h post dose. Animal Model: Heterozygote Q175DN KI mouse model of HD [1] Dosage: 10 mg/kg Administration: Oral adiministration; 10 mg/kg; twice a day; 90 days Result: Led to lower-than-expected brain concentrations compared to single dosing. |
分子量 | 372.44 |
分子式 | C20H25FN4O2 |
CAS No. | 2573071-18-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Rho-Kinase-IN-2 2573071-18-6 Inhibitor inhibitor inhibit