2017年11月30日星期四

Y-33075 dihydrochloride|cas: 173897-44-4

Y-33075 dihydrochloride|cas: 173897-44-4

DC Chemicals, Website: www.dcchemicals.com

Product Name: Y-33075 dihydrochloride|Cas Number: 173897-44-4| Catalog Number: DC10351|Other Nmaes: Y39983 hydrochlorid

Y-33075 dihydrochloride is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632.

In the examination of inhibition of PKC and CaMKII, the IC50s of Y-27632 and Y-39983 for PKC is 9.0 μM and 0.42 μM, respectively, whereas the IC50s of Y-27632 and Y-39983 for CaMKII is 26 μM and 0.81 μM, respectively. The IC50s of Y-27632 and Y-39983 for PKC is 82 and 117 times those for ROCK, respectively, whereas the IC50s of Y-27632 and Y-39983 for CaMKII is 236 and 225 times those for ROCK, respectively[1]. Y-39983 (10 μM) extends neurites in the RGCs compared with those in RGCs treated without Y-39983[2].In rabbits and in monkeys, Y-39983 lowers IOP in a dose-dependent fashion[1]. An increase in regenerating axons of RGCs in 100 mM Y-39983-treated eyes is observed compared with saline-treated eyes. Y-39983 dose-dependently increases the number of RGCs with regenerating axons[2]. Both Y-27632 and Y-39983 induces a concentration-dependent relaxation in rabbit ciliary arteries precontracted with a high-potassium (high-K) solution. The amplitude of relaxation induced by Y-27632 and Y-39983 is not affected by either 100 μM N (G)-nitro-L: -arginine methyl ester (L: -NAME) or 10 μM indomethacin. In Ca2+-free solution, Y-27632 and Y-39983 significantly inhibits the transient contraction of ciliary arteries induced by 10 μM histamine. However, neither Y-27632 nor Y-39983 affects the elevation of [Ca2+](i) induced by high-K solution and histamine[3].

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