AS 1892802
- Product Name
- AS 1892802
- CAS No.
- 928320-12-1
- Chemical Name
- AS 1892802
- 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]-
- CBNumber
- CB73146254
- Molecular Formula
- C20H19N3O2
- Formula Weight
- 333.38
- MOL File
- 928320-12-1.mol
AS 1892802 Property
- 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
N-Bromosuccinimide Price
- Product number
- 14978
- Product name
- AS-1892802
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 14978
- Product name
- AS-1892802
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 14978
- Product name
- AS-1892802
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $257
- Updated
- 2024/03/01
- Product number
- 14978
- Product name
- AS-1892802
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $586
- Updated
- 2024/03/01
- Product number
- 4927
- Product name
- AS1892802
- Purity
- ≥99%(HPLC)
- Packaging
- 50
- Price
- $821
- Updated
- 2021/12/16
AS 1892802 Chemical Properties,Usage,Production
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.
AS 1892802 Preparation Products And Raw materials
Raw materials
Preparation Products
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