Y-33075 dihydrochloride

SKU: orb1219732

描述

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.

图片与验证

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关键属性

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CAS 号	173897-44-4
MW	353.25
纯度	>98% (HPLC)
分子式	C₁₆H₁₈Cl₂N₄O
SMILES	Cl.Cl.C[C@@H](N)c1ccc(cc1)C(=O)Nc1ccnc2[nH]ccc12
靶点	ROCK
溶解性	DMSO:100 mg/mL (283.09 mM; Need ultrasonic);H2O:50 mg/mL (141.54 mM; Need ultrasonic)

生物活性

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体内

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.

体外

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.

储存与操作

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储存	Storage temperature: -20°C. Stability: ≥ 2 years
有效期	12 months from date of receipt.
免责声明	For research use only

相似产品

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Y-33075 dihydrochloride [orb1308924]
纯度：
99.89% (May vary between batches)
CAS 号：
173897-44-4
MW:
353.25
分子式：
C₁₆H₁₈Cl₂N₄O
可选规格： 5 mg, 10 mg, 50 mg, 100 mg, 25 mg, 1 mg, 200 mg, 1 ml x 10 mM (in DMSO)

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常用数据库链接

基因符号

ROCK

实验方案信息

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