AS 1892802 Struktur

AS 1892802

Bezeichnung:AS 1892802

CAS-Nr928320-12-1

Englisch Name:AS 1892802

CBNumberCB73146254

SummenformelC20H19N3O2

Molgewicht333.38

MOL-Datei928320-12-1.mol

AS 1892802 physikalisch-chemischer Eigenschaften

Siedepunkt	531.2±50.0 °C(Predicted)
Dichte	1.256±0.06 g/cm3(Predicted)
storage temp.	Store at RT
Löslichkeit	Soluble in DMSO
Aggregatzustand	crystalline solid
pka	12.42±0.46(Predicted)

AS 1892802 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
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.
Biologische Aktivität
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].
Einzelnachweise
[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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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