CAS NO: | 199433-58-4 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | Y-33075 is a selectiveROCKinhibitor derived from Y-27632, and is more potent than Y-27632, with anIC50of 3.6 nM. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Y-33075 (Y-39983) is a potent ROCK inhibitor, with an IC50of 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[1]. Y-33075 (Y-39983, 10 μM) extends neurites in the retinal ganglion cells (RGCs) compared with those in RGCs treated without Y-39983[2]. 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[3]. | ||||||||||||||||
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[1]. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats[2]. | ||||||||||||||||
分子量 | 280.32 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C16H16N4O | ||||||||||||||||
CAS 号 | 199433-58-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | 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℃) 配制储备液
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以下溶剂前显示的百
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