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Purity: ≥98%
Y-39983 HCl (also called Y-33075) is a novel, potent and selective inhibitor of Rho-associated coiled coil-forming protein kinase( ROCK ) with IC50 values of 3.6 nM, 0.42 μM and 0.81 μM for ROCK, PKC and CaMKII, respectively. Y-39983 acts by downregulating RhoA/Rho-associated kinase expression during its promotion of axonal regeneration. Y-39983 also promotes regeneration of crushed axons of retinal ganglion cells into the optic nerve of adult cats. Y-39983 has been reported to relax the ciliary arteries of precontracted isolated rabbit in vitro. In addition, Y-39983 has been found to increase optic-nerve-head blood flow by laser speckle flowmetry. Moreover, Y-39983 lowered the intraocular pressure ( IOP) in a dose-dependent fashion in the eyes of rabbits and monkeys.
| ln Vitro |
Y-33075, also known as Y-39983, is a strong inhibitor of ROCK, with an IC50 of 3.6 nM. Furthermore, Y-33075 inhibits PKC and CaMKII more potently than Y-27632. Y-27632 and Y-33075 had IC50 values of 9.0 μM and 0.42 μM against PKC and 26 μM and 0.81 μM, respectively, against CaMKII. Y-27632 and Y-33075 had IC50s of 82 and 117 times that of ROCK against PKC, and 236 and 225 times that of ROCK against CaMKII, respectively [1]. In comparison to neurites in RGCs not receiving Y-39983 therapy, Y-33075 (Y-39983, 10 μM) lengthens them in RGCs [2]. Rabbit ciliary artery segments in a Ca2+-free solution are not able to contract due to histamine when exposed to Y-33075 (Y-39983, 1 μM). In solutions with high potassium (high K), Y-33075 (10 μM) does not affect the rise in [Ca2+]i [3].
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| ln Vivo |
Y-39983 (≥0.01%) dramatically reduces intraocular pressure (IOP) in rabbits two hours after topical application. IOP significantly decreases in monkeys' treated eyes with Y-39983 (0.05%) between two and seven hours after topical application. management[1]. Rat eyes with retinal ganglion cells (RGCs) have more regenerating axons when exposed to 100 μM Y-39983[2].
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| References |
[1]. Hideki Tokushige, et al. Effects of Topical Administration of Y-39983, a Selective Rho-Associated Protein Kinase Inhibitor, on Ocular Tissues in Rabbits and Monkeys Invest. Ophthalmol. Vis. Sci. July 2007 vol. 48no. 7 3216-3222
[2]. Tokushige H, et al. Effects of Y-39983, a selective Rho-associated protein kinase inhibitor, on blood flow in optic nerve head in rabbits and axonal regeneration of retinal ganglion cells in rats. Curr Eye Res. 2011 Oct;36(10):964-70. [3]. Watabe H, et al. Effects of Rho-associated protein kinase inhibitors Y-27632 and Y-39983 on isolated rabbit ciliary arteries.Jpn J Ophthalmol. 2011 Jul;55(4):411-7. Epub 2011 Jun 11 |
| Molecular Formula |
C16H18CL2N4O
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| Molecular Weight |
353.25
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| CAS # |
173897-44-4
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| Related CAS # |
Y-33075;199433-58-4;Y-33075 hydrochloride;471843-75-1
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| SMILES |
O=C(C1C=CC([C@@](C)(N)[H])=CC=1)NC1C=CN=C2NC=CC=12.[H]Cl.[H]Cl
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 30 mg/mL Solubility in Formulation 5: 100 mg/mL (283.09 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8309 mL | 14.1543 mL | 28.3086 mL | |
| 5 mM | 0.5662 mL | 2.8309 mL | 5.6617 mL | |
| 10 mM | 0.2831 mL | 1.4154 mL | 2.8309 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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