AS 1892802 CAS: 928320-12-1
MF: C20H19N3O2
MW: 333.38
An ATP-competitive ROCK inhibitor.

AS 1892802 (CAS 928320-12-1)

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Alternate Names: AS1892802; AS-1892802
Application: AS 1892802 is an ATP-competitive ROCK inhibitor
CAS Number: 928320-12-1
Molecular Weight: 333.38
Molecular Formula: C20H19N3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

AS 1892802 is a potent, ATP-competitive ROCK inhibitor with IC50 values of 52, 57 and 122 nM for human ROCK2, rat ROCK2 and human ROCK1, respectively. In rat models, AS 1892802 has been shown to prevent the formation of tibial cartilage lesions due to MIA induction of osteoarthritis.


References

R. Li et al. Fragment-Based and Structure-Guided Discovery and Optimization of Rho Kinase Inhibitors. J. Med. Chem. 2012, 55, 2474−2478.

N. Takeshita et al. Alleviating Effects of AS1892802, a Rho Kinase Inhibitor, on Osteoarthritic Disorders in Rodents. J. Pharmacol. Sci. 2011, 115, 481–489.

E. Yoshimi 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, 955-963.

E. Yoshimi et al. Sustained analgesic effect of the Rho kinase inhibitor AS1892802 in rat models of chronic pain. J. Pharmacol. Sci. 2010, 114, 119-122.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (25 mM).
Storage :
Store at 4° C
Boiling Point :
~531.2° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
Optical Activity :
α20/D +85.8°, c = 0.68 in methanol
IC50 :
ROCK2: IC50 = 52 nM (human); ROCK2: IC50 = 57 nM (rat); ROCK1: IC50 = 122 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
46911016
SMILES :
C1=CC=C(C=C1)[[email protected]@H](CO)NC(=O)NC2=CC=C(C=C2)C3=CC=NC=C3

Download SDS (MSDS)

Certificate of Analysis

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