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CAS No. : 173897-44-4
MCE 国际站:Y-33075 dihydrochloride
产品活性:Y-33075 dihydrochloride是选择性的 ROCK 抑制剂,IC50 为 3.6 nM。
研究领域:Cell Cycle/DNA Damage | Stem Cell/Wnt | Cytoskeleton | TGF-beta/Smad
作用靶点:ROCK
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 Ca2+-free solutions. Y-33075 (10 μM) shows no effect on the [Ca2+]i increase with the high-potassium (high-K) solution.
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.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | TGF-beta/Smad Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Cytoskeleton Compound Library | FDA Approved & Pharmacopeial Drug Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Chroman 1 dihydrochloride | Ripasudil free base | AS1892802 | Hu7691 free base | Sovesudil | AT13148 | CRT0066854 | LX7101 | Y-27632 dihydrochloride | RKI-1447 | HA-100 hydrochloride | WF-536 | Pentanoic acid-d9 | Fasudil dihydrochloride | ROCK-IN-5 | ROCK2-IN-5 | BDP5290 | PF-4950834 | PT-262 | Afuresertib hydrochloride | Belumosudil mesylate | GSK429286A | Y-27632 dihydrochloride (GMP) | H-1152 dihydrochloride | 3-(4-Pyridyl)indole | ROCK inhibitor-2 | ROCK-IN-7 | ZINC00881524
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