Rho-Kinase-IN-2
目录号 : GC66050
Rho-Kinase-IN-2 (Compound 23) 是一种具有口服活性的、选择性的和中枢神经系统 (CNS) 渗透性的 Rho激酶 (ROCK) 抑制剂 (ROCK2 IC50=3 nM)。Rho-Kinase-IN-2 可用于亨廷顿病的研究。
Cas No.:2573071-18-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington's research[1].
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 (EC50=28 nM) and a decrease in MYPT1 phosphorylation (IC50=14 nM). |
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 IC50=∼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 IC50 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. |
| Cas No. | 2573071-18-6 | SDF | Download SDF |
| 分子式 | C20H25FN4O2 | 分子量 | 372.44 |
| 溶解度 | DMSO : 50 mg/mL (134.25 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.685 mL | 13.425 mL | 26.85 mL |
| 5 mM | 0.537 mL | 2.685 mL | 5.37 mL |
| 10 mM | 0.2685 mL | 1.3425 mL | 2.685 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。