Y-33075 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Y-33075 diHClide 是一种选择性 ROCK 抑制剂（IC50 为 3.6 nM）。Y-33075 (Y-39983) 是一种有效的 ROCK 抑制剂（IC50 为 3.6 nM）。 Y-33075 还比 Y-27632 更有效地抑制 PKC 和 CaMKII（Y-27632 和 Y-33075 对 PKC 的 IC50 分别为 9.0 μM 和 0.42 μM），而 Y-27632 和 Y-33075 对 CaMKII 的 IC50 为分别为 26 μM 和 0.81 μM。

Y-33075 dihydrochloride is a selective inhibitor of ROCK(IC50 of 3.6 nM).Y-33075 (Y-39983) is a potent inhibitor of ROCK(IC50 of 3.6 nM). Y-33075 also inhibits PKC and CaMKII more potently than Y-27632(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 Ca2+-free solutions.Y-39983 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration in rabbits. Y-39983 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration in monkeys. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats.

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 Ca2+-free solutions. Y-33075 (10 μM) shows no effect on the [Ca2+]i increase with the high-potassium (high-K) solution.

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.

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Cell Cycle/DNA Damage

ROCK

ROCK|PKC|CaMKII

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173897-44-4

353.25

C16H18Cl2N4O

>98% (HPLC)

DMSO:100 mg/mL (283.09 mM; Need ultrasonic);H2O:50 mg/mL (141.54 mM; Need ultrasonic)

Cl.Cl.C[C@@H](N)c1ccc(cc1)C(=O)Nc1ccnc2[nH]ccc12

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(-20℃)

With Ice Pack

≥ 2 years