(R)-4-(1-aMinoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzaMide dihydrochloride Chemical Properties

storage temp. 

Inert atmosphere,Room Temperature

solubility 

Soluble in DMSO

form 

Solid

color 

White to gray

optical activity

[α]/D +5 to +9°, c =1 in methanol

InChI

InChI=1/C16H16N4O.2ClH/c1-10(17)11-2-4-12(5-3-11)16(21)20-14-7-9-19-15-13(14)6-8-18-15;;/h2-10H,17H2,1H3,(H2,18,19,20,21);2*1H/t10-;;/s3

InChIKey

CKFHAVRPVZNMGT-WTVPDBJGNA-N

SMILES

C(NC1C=CN=C2NC=CC2=1)(=O)C1=CC=C([C@H](N)C)C=C1.Cl.Cl |&1:16,r|

(R)-4-(1-aMinoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzaMide dihydrochloride Usage And Synthesis

Uses

Y-39983 Hydrochloride contain Rho kinase inhibitory activity.

Biological Activity

y-39983 dihydrochloride is a novel and selective inhibitor of rock family with ic50 value of 3.6nm for rock [1].y-39983 dihydrochloride has shown a selective inhibitor of rho-associated coiled coil-forming protein kinase( rock ) with ic50 values of 3.6nm, 0.42μm and 0.81μm for rock, pkc and camkii, respectively [1]. apart from these, y-39983 has been reported to relax the ciliary arteries of precontracted isolated rabbit in vitro. in addition, y-39983 has been found to increase optic-nerve-head blood flow by laser speckle flowmetry [2]. moreover, y-39983 lowered the intraocular pressure ( iop) in a dose-dependent fashion in the eyes of rabbits and monkeys [1].

in vivo

IC 50

ROCK: 3.6 nM (IC₅₀); PKC: 420 nM (IC₅₀); CaMKII: 810 nM (IC₅₀)

References

[1] tokushige h1, inatani m, nemoto s, sakaki h, katayama k, uehata m, tanihara h. effects of topical administration of y-39983, a selective rho-associated protein kinase inhibitor, on ocular tissues in rabbits and monkeys. invest ophthalmol vis sci. 2007 jul;48(7):3216-22.
[2] watabe h1, abe s, yoshitomi t. effects of rho-associated protein kinase inhibitors y-27632 and y-39983 on isolated rabbit ciliary arteries. jpn j ophthalmol. 2011 jul;55(4):411-7. doi: 10.1007/s10384-011-0048-9. epub 2011 jun 11.

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