| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 0.014 μM (ROCK I); 0.003 μM (ROCK II)[1]
CAY10746 targets Rho-associated kinases I and II (ROCK I and ROCK II), which are serine/threonine kinases involved in the regulation of the actin cytoskeleton, cell adhesion, migration, and proliferation. The compound inhibits ROCK I with an IC50 of 0.014 μM (14 nM) and ROCK II with an IC50 of 0.003 μM (3 nM). It is selective for ROCK over PKA (IC50 > 10 μM). ROCK inhibition has therapeutic potential in diabetic retinopathy and other diseases. |
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| ln Vitro |
Compound 12j, also known as CAY10746, exhibits inhibitory activity against both ROCK I and II, with IC50 values of 0.014 μM and 0.003 μM, in that order [1]. CAY10746 suppresses ROCK kinase activity in SH-SY5Y cells at concentrations of 0.1, 1, and 10 μM; 0.25, 1, 2, and 4 hours [1]. In vitro, CAY10746 (1 μM; 24 h, 36 h) inhibits the migration of endothelial cells [1]. Retinal neurons are shielded from oxidative stress and cell death caused by apoptosis by CAY10746 (1 μM; 5 days) [1]. Retinal explants grown in a high-glucose milieu show that CAY10746 (1 μM; 5 days) increases vascular degeneration and prevents improper Müller cell proliferation [1].
In vitro studies demonstrate that CAY10746 exhibits inhibitory activity against ROCK I and ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. The compound is selective for ROCK over PKA (IC50 > 10 μM). CAY10746 is a selective Rho kinase (ROCK) inhibitor. The compound can be used in the study of diabetic retinopathy. |
| ln Vivo |
No detailed in vivo activity data has been published for CAY10746. The compound is a selective ROCK inhibitor that can be used in the study of diabetic retinopathy (DR). ROCK inhibition has been shown to have therapeutic potential in various diseases including diabetic retinopathy, glaucoma, and cardiovascular diseases. Further studies would be needed to evaluate the in vivo efficacy of CAY10746 in these disease models.
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| Enzyme Assay |
The ROCK inhibitory activity of CAY10746 can be assessed using in vitro kinase assays. In a typical assay, recombinant ROCK I or ROCK II kinase is incubated with a peptide substrate, ATP (including radiolabeled ³³P-ATP), and varying concentrations of CAY10746. The incorporation of phosphate into the substrate is measured, and the IC50 is calculated. The IC50 for ROCK I is 0.014 μM and for ROCK II is 0.003 μM. The selectivity against PKA is assessed using similar assays.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: SH-SY5Y cells Tested Concentrations: 0.1, 1 and 10 μM; 10 μM Incubation Duration: 2 h; 0.25, 1, 2 and 4 h Experimental Results: Inhibited the phosphorylation of MYPT1 but did not impact the MYPT1 expression in dose-dependence and time-dependence. Cell Proliferation Assay[1] Cell Types: SH-SY5Y cells Tested Concentrations: 1 μM Incubation Duration: 5 days Experimental Results: Dramatically protected the cells from death. Cell Migration Assay [1] Cell Types: HUVEC cells Tested Concentrations: 1 μM Incubation Duration: 24 h, 36 h Experimental Results: Dramatically decreased migrating cell numbers and Dramatically reduce the rate of wound healing at 24 h and 36 h. Apoptosis Analysis[1] Cell Types: ex vivo DR model Tested Concentrations: 1 μM Incubation Duration: 5 days Experimental Results: Dramatically protected neuronal cells from death. The cellular activity of CAY10746 is assessed using cell-based assays that measure ROCK activity. Cells are treated with varying concentrations of CAY10746. ROCK activity is assessed by measuring phosphorylation of ROCK substrates such as myosin light chain (MLC) or cofilin by Western blotting using phospho-specific antibodies. Cell migration and adhesion assays can be used to assess functional effects of ROCK inhibition. Cell viability is measured using MTT assays. |
| Animal Protocol |
No detailed in vivo animal model data has been published for CAY10746. The compound has been suggested for use in the study of diabetic retinopathy (DR). Future studies may involve the use of mouse models of diabetic retinopathy or other ROCK-related diseases to assess the in vivo efficacy of CAY10746. Such studies would be essential to confirm the compound's therapeutic potential.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published for CAY10746. The compound has a molecular weight of 457.48 g/mol and a molecular formula of C26H23N3O5. The compound has a purity of 98.61%. Further studies would be needed to characterize its absorption, distribution, metabolism, and excretion properties, including oral bioavailability, plasma protein binding, clearance, and half-life.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for CAY10746. As a ROCK inhibitor, it may have on-target effects on vascular and smooth muscle function. Comprehensive toxicology studies would be required to evaluate its safety profile for potential therapeutic development. The compound is intended for research use only.
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| References | |
| Additional Infomation |
CAY10746 (CAS# 2247240-76-0) is a selective Rho kinase (ROCK) inhibitor with IC50 values of 0.014 μM for ROCK I and 0.003 μM for ROCK II. It is selective for ROCK over PKA (IC50 > 10 μM). CAY10746 can be used in the study of diabetic retinopathy (DR). The molecular formula is C26H23N3O5 and molecular weight is 457.48 g/mol. The compound has a purity of 98.61%.
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| Molecular Formula |
C26H23N3O5
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|---|---|
| Molecular Weight |
457.48
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| Exact Mass |
457.163
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| CAS # |
2247240-76-0
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
664.2±55.0 °C at 760 mmHg
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| Flash Point |
355.5±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.697
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| LogP |
3.26
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : 83.33 mg/mL (182.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.55 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 20.8 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: ≥ 2.08 mg/mL (4.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1859 mL | 10.9294 mL | 21.8589 mL | |
| 5 mM | 0.4372 mL | 2.1859 mL | 4.3718 mL | |
| 10 mM | 0.2186 mL | 1.0929 mL | 2.1859 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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