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 . 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 . AS 1892802 is a potent ROCK inhibitor. AS 1892802 inhibited ROCK1 and ROCK2 with IC50 values of 1.69 and 0.10 μM, respectively . In ATDC5 cells, AS1892802 induce chondrocyte differentiation. In HIG82 cells, AS1892802 significantly inhibited prostaglandin E2 production induced by IL-1β or bradykinin . 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 . In monoiodoacetate-induced arthritis and streptozotocin-induced neuropathy models, AS1892802 showed analgesic effect . 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 .

Product information

CAS Number: 928320-12-1

Molecular Weight: 333.38

Formula: C20H19N3O2

Chemical Name: (Z,1S)-2-hydroxy-1-phenyl-N-[4-(pyridin-4-yl)phenyl]ethane-1-carbamimidic acid

Smiles: O/C(/NC1C=CC(=CC=1)C1=CC=NC=C1)=N\[C@H](CO)C1C=CC=CC=1

InChiKey: WDTFYYZHMRBVHK-LJQANCHMSA-N

InChi: InChI=1S/C20H19N3O2/c24-14-19(17-4-2-1-3-5-17)23-20(25)22-18-8-6-15(7-9-18)16-10-12-21-13-11-16/h1-13,19,24H,14H2,(H2,22,23,25)/t19-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.