CAY10746
Based on 1 publication(s) in Google Scholar
CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.61%
- No. CAS: 2247240-76-0
- Fòrmula: C26H23N3O5
- Peso molecular:457.48
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CAY10746
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 0.014 μM (ROCK I); 0.003 μM (ROCK II)[1]
In Vitro
CAY10746 (compound 12j) has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively[1].
CAY10746 (0.1, 1 and 10 μM; 0.25, 1, 2 and 4 h) inhibits ROCK kinase activity in SH-SY5Y cells[1].
CAY10746 (1 μM; 24 h, 36 h) inhibits endothelial cell migration in vitro[1].
CAY10746 (1 μM; 5 days) protects retinal neurons from high glucose-induced oxidative stress and apoptosis-mediated cell death[1].
CAY10746 (1 μM; 5 days) suppresses the improper proliferation of Müller cells and promoted the regression of vascular vessels in retinal explants cultured in a high glucose microenvironment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:SH-SY5Y cells
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Concentration:0.1, 1 and 10 μM; 10 μM
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Incubation Time:2 h; 0.25, 1, 2 and 4 h
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Result:Inhibited the phosphorylation of MYPT1 but did not impact the MYPT1 expression in dose-dependence and time- dependence.
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Cell Line:SH-SY5Y cells
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Concentration:1 μM
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Incubation Time:5 days
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Result:Significantly protected the cells from death.
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Cell Line:HUVEC cells
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Concentration:1 μM
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Incubation Time:24 h, 36 h
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Result:Significantly reduced migrating cell numbers and significantly reduce the rate of wound healing at 24 h and 36 h.
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Cell Line:ex vivo DR model
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Concentration:1 μM
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Incubation Time:5 days
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Result:Significantly protected neuronal cells from death.
Chemical Information
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No. CAS 2247240-76-0
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Appearance Solid
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Peso molecular 457.48
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Fòrmula C26H23N3O5
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Color Off-white to light yellow
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SMILES
O=C1C=COC2=CC(OCC(NC3=CC(NC(C4=CC=C(N(C)C)C=C4)=O)=CC=C3)=O)=CC=C12
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Curr Eye Res
Topical CAY-10746, a Novel ROCK Inhibitor, Reduces Intraocular Pressure and Modulates the Trabecular Meshwork in Normotensive Rats. [Abstract]2026 May 7:1-11. PMID: 42095348
Solvente y solubilidad
In Vitro:
DMSO : 83.33 mg/mL (182.15 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1859 mL | 10.9294 mL | 21.8589 mL | 54.6472 mL |
| 5 mM | 0.4372 mL | 2.1859 mL | 4.3718 mL | 10.9294 mL | |
| 10 mM | 0.2186 mL | 1.0929 mL | 2.1859 mL | 5.4647 mL | |
| 15 mM | 0.1457 mL | 0.7286 mL | 1.4573 mL | 3.6431 mL | |
| 20 mM | 0.1093 mL | 0.5465 mL | 1.0929 mL | 2.7324 mL | |
| 25 mM | 0.0874 mL | 0.4372 mL | 0.8744 mL | 2.1859 mL | |
| 30 mM | 0.0729 mL | 0.3643 mL | 0.7286 mL | 1.8216 mL | |
| 40 mM | 0.0546 mL | 0.2732 mL | 0.5465 mL | 1.3662 mL | |
| 50 mM | 0.0437 mL | 0.2186 mL | 0.4372 mL | 1.0929 mL | |
| 60 mM | 0.0364 mL | 0.1822 mL | 0.3643 mL | 0.9108 mL | |
| 80 mM | 0.0273 mL | 0.1366 mL | 0.2732 mL | 0.6831 mL | |
| 100 mM | 0.0219 mL | 0.1093 mL | 0.2186 mL | 0.5465 mL |
CAY10746 Related Classifications
HY-139170 Related Classifications
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