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KI2525AS189280210 mg$585
AS189280250 mg$2457

Chemical Characteristic

Product NameAS1892802
SynonymsN/A
CAS No.928320-12-1
Molecular Weight 333.38
FormulaC20H19N3O2
Chemical NameN-[(1S)-2-Hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]-urea
SmilesN(C(=O)Nc1ccc(cc1)c1ccncc1)C(CO)c1ccccc1
Chemical Structure

Biological activities

AS1892802 is a novel and highly selective Rho kinase (ROCK) inhibitor. AS1892802 potently inhibits human ROCK1 (hROCK1), hROCK2, and rat ROCK2 (rROCK2) with IC50s of 122, 52 and 57 nM, respectively. AS1892802 diminishes the inhibition of CYP isoforms for 3A4, 2D6, 1A2, 2C9, and 2C19 with IC50s of 15, 17, 25, 13, and 19 μM, respectively.[1] AS1892802 inhibits IL-1β??nduced PGE2 production in a synovial cell line.[2] Orally administered AS1892802 exhibits potent antinociceptive effect in an adjuvant-induced arthritis (AIA) model (inflammatory arthritis model). Orally administered AS1892802 exhibits potent antinociceptive effect in a monoiodoacetate-induced arthritis (MIA) model (noninflammatory arthritis model), with an ED50 of 0.15 mg/kg (MIA model).[1]

Protocols

In vivo, AS1892802 is dissolved in distilled water.[1]

References

[1] Yoshimi E, 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] Takeshita N, 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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