928320-12-1 Usage
Description
AS 1892802 is a potent, ATP-competitive Rho-associated coiled-coil containing protein kinase (ROCK) inhibitor. It also inhibits protein kinase A catalytic subunit alpha (PKAC-α) and protein kinase X-linked (PRKX). AS 1892802 has been found to exhibit analgesic effects in rat models of inflammatory and noninflammatory arthritic pain.
Uses
Used in Pharmaceutical Industry:
AS 1892802 is used as a ROCK inhibitor for its potential therapeutic applications in treating inflammatory and noninflammatory arthritic pain. Its ability to inhibit PKAC-α and PRKX, along with its analgesic effects, makes it a promising candidate for the development of new treatments for pain management.
Used in Pain Management:
AS 1892802 is used as an analgesic agent for its ability to alleviate pain in rat models of inflammatory (AIA) and noninflammatory (MIA) arthritic pain. Its multi-targeted inhibition of ROCK, PKAC-α, and PRKX may contribute to its pain-relieving properties, offering a potential new approach to managing arthritic pain and other pain-related conditions.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 928320-12-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,2,8,3,2 and 0 respectively; the second part has 2 digits, 1 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 928320-12:
(8*9)+(7*2)+(6*8)+(5*3)+(4*2)+(3*0)+(2*1)+(1*2)=161
161 % 10 = 1
So 928320-12-1 is a valid CAS Registry Number.
928320-12-1Relevant articles and documents
INHIBITORS OF RHO ASSOCIATED PROTEIN KINASES (ROCK) AND METHODS OF USE
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Page/Page column 45; 46, (2013/08/15)
Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.
NOVEL COMPOUNDS
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Page/Page column 64, (2008/06/13)
This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
