AS 1892802
目录号 : GC11754
A ROCK1 and ROCK2 inhibitor
Cas No.:928320-12-1
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
AS 1892802 is a potent and selective inhibitor of ROCK with IC50 values of 52, 57 and 122 nM for human ROCK2, rat ROCK2 and human ROCK1, respectively [1].
Rho kinase (ROCK) is a serine-threonine kinase and is a downstream effector of Rho, a small GTP-bound protein. ROCK phosphorylates target proteins such as myosin light chain kinase and LIM kinase and regulates cellular shape modification, migration, growth and contraction [2].
AS 1892802 is a potent ROCK inhibitor. AS 1892802 inhibited ROCK1 and ROCK2 with IC50 values of 1.69 and 0.10 μM, respectively [3]. In ATDC5 cells, AS1892802 induce chondrocyte differentiation. In HIG82 cells, AS1892802 significantly inhibited prostaglandin E2 production induced by IL-1β or bradykinin [4].
In both an adjuvant-induced arthritis (AIA) rat model and a monoiodoacetate (MIA) -induced arthritis (MIA) rat model, AS1892802 showed potent antinociceptive effect with ED50 value of 0.15 mg/kg [1]. In monoiodoacetate-induced arthritis and streptozotocin-induced neuropathy models, AS1892802 showed analgesic effect [2]. In MIA-injected rats, the mRNA levels of ROCK I and II increased in knee joints. AS1892802 significantly inhibited cartilage damage in a dose-dependent way [4].
References:
[1]. Yoshimi E, Kumakura F, Hatori C, et al. Antinociceptive effects of AS1892802, a novel Rho kinase inhibitor, in rat models of inflammatory and noninflammatory arthritis. J Pharmacol Exp Ther, 2010, 334(3): 955-963.
[2]. Yoshimi E, Yamamoto H, Furuichi Y, et al. Sustained analgesic effect of the Rho kinase inhibitor AS1892802 in rat models of chronic pain. J Pharmacol Sci, 2010, 114(1): 119-122.
[3]. Li R, Martin MP, Liu Y, et al. Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors. J Med Chem, 2012, 55(5): 2474-2478.
[4]. Takeshita N, Yoshimi E, Hatori C, et al. Alleviating effects of AS1892802, a Rho kinase inhibitor, on osteoarthritic disorders in rodents. J Pharmacol Sci, 2011, 115(4): 481-489.
| Cas No. | 928320-12-1 | SDF | |
| 化学名 | (S,Z)-N'-(2-hydroxy-1-phenylethyl)-N-(4-(pyridin-4-yl)phenyl)carbamimidic acid | ||
| Canonical SMILES | OC[C@](/N=C(O)/NC1=CC=C(C2=CC=NC=C2)C=C1)([H])C3=CC=CC=C3 | ||
| 分子式 | C20H19N3O2 | 分子量 | 333.38 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 25 mg/ml,DMSO:PBS (pH 7.2) (1:7): 0.12 mg/ml | 储存条件 | Store at RT |
| 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 | 2.9996 mL | 14.9979 mL | 29.9958 mL |
| 5 mM | 0.5999 mL | 2.9996 mL | 5.9992 mL |
| 10 mM | 0.3 mL | 1.4998 mL | 2.9996 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。