| Identification | Back Directory | [Name]
AS 1892802 | [CAS]
928320-12-1 | [Synonyms]
AS 1892802
N-[(1S)-2-Hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]-urea
Urea, N-[(1S)-2-hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]- | [Molecular Formula]
C20H19N3O2 | [MDL Number]
MFCD26792591 | [MOL File]
928320-12-1.mol | [Molecular Weight]
333.38 |
| Chemical Properties | Back Directory | [Boiling point ]
531.2±50.0 °C(Predicted) | [density ]
1.256±0.06 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
Soluble in DMSO | [form ]
crystalline solid | [pka]
12.42±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
AS 1892802 is a potent, ATP-competitive ROCK inhibitor. It also inhibits PKAC-α and PRKX and exhibits analgesic effects in rat models of inflammatory (AIA) and noninflammatory (MIA) arthritic pain. | [Biological Activity]
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. |
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http://www.approvedhomemanagement.com/ShowSupplierProductsList112975/0.htm |
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