Y 33075;4-[(1R)-1-Aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide;Y 39983;Y-33075;CHEBI:674917;CHEMBL571948;CS-0097;HY-10067;KB-81516;SureCN226556;Y-39983;(R)-4-(1-Aminoethyl)-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide
Cas No.
199433-58-4
分子式
C16H16N4O
分子量
280.32
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Y-33075 是一种有效的 ROCK 抑制剂,源于 Y-27632,但活性更强,IC50 值 3.6 nM。
生物活性
Y-33075 is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC 50 of 3.6 nM.
性状
Solid
IC50 & Target[1][2]
ROCK 3.6 nM (IC50) PKC 420 nM (IC50
体外研究(In Vitro)
Y-33075 (Y-39983) is a potent ROCK inhibitor, with an IC50 of 3.6 nM. Y-33075 also inhibits PKC and CaMKII more potently than Y-27632, and the IC50s of Y-27632 and Y-33075 for PKC are 9.0 μM and 0.42 μM, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII are 26 μM and 0.81 μM, respectively. The IC50s of Y-27632 and Y-33075 for PKC is 82 and 117 times those for ROCK, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII is 236 and 225 times those for ROCK, respectively. Y-33075 (Y-39983, 10 μM) extends neurites in the retinal ganglion cells (RGCs) compared with those in RGCs treated without Y-39983. Y-33075 (Y-39983, 1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca-free solutions. Y-33075 (10 μM) shows no effect on the [Ca]i increase with the high-potassiu
体内研究(In Vivo)
In rabbits, Y-39983 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration. In monkeys, Y-39983 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Hideki Tokushige, et al. 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. July 2007 vol. 48no. 7 3216-3222[2]. Tokushige H, et al. Effects of Y-39983, a selective Rho-associated protein kinase inhibitor, on blood flow in optic nerve head in rabbits and axonal regeneration of retinal ganglion cells in rats. Curr Eye Res. 2011 Oct;36(10):964-70.
溶解度数据
In Vitro: DMSO : 50 mg/mL (178.37 mM; Need ultrasonic and warming)H2O : 1 mg/mL (3.57 mM; ultrasonic and heat to 60°C)配制储备液