AS 1892802
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AS1892802是ROCK的强效选择性抑制剂,对人ROCK2\大鼠ROCK2和人ROCK1的IC50值分别为52\57和122 nM[1].
Rho激酶(ROCK)是一种丝氨酸-苏氨酸激酶,是小GTP结合蛋白Rho的下游效应子.ROCK磷酸化靶蛋白,例如肌球蛋白轻链激酶和LIM激酶,调节细胞形状改变\迁移\生长和收缩[2].
AS1892802是一种强效的ROCK抑制剂.AS1892802抑制ROCK1和ROCK2的IC50值分别为1.69和0.10 μM[3].在ATDC5细胞中,AS1892802诱导细胞分化.在HIG82细胞中,AS1892802显著抑制IL-1β或缓激肽诱导的前列腺素E2生成[4].
在免疫佐剂诱导的关节炎(AIA)大鼠模型和monoiodoacetate诱导的关节炎(MIA)大鼠模型中,AS1892802表现出强效的镇痛作用,ED50值为0.15 mg/kg[1].在monoiodoacetate诱导的关节炎和链脲佐菌素诱导的神经病模型中,AS1892802具有镇痛作用[2].在MIA注射的大鼠中,膝关节中ROCK I和II的mRNA表达水平增加.AS1892802以剂量依赖的方式显著抑制软骨损伤[4].
参考文献:
[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 Pharmaco
Physical Appearance | A crystalline solid |
Storage | Store at RT |
M.Wt | 333.38 |
Cas No. | 928320-12-1 |
Formula | C20H19N3O2 |
Solubility | Soluble in DMSO |
Chemical Name | (S,Z)-N'-(2-hydroxy-1-phenylethyl)-N-(4-(pyridin-4-yl)phenyl)carbamimidic acid |
SDF | Download SDF |
Canonical SMILES | OC[C@](/N=C(O)/NC1=CC=C(C2=CC=NC=C2)C=C1)([H])C3=CC=CC=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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