| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
IC50: 0.014 μM (ROCK I); 0.003 μM (ROCK II)[1]
|
|---|---|
| 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].
|
| 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. |
| References |
[1]. Lanying Zhao, et al. Discovery of 4 H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models. J Med Chem. 2019 Dec 12;62(23):10691-10710.
|
| Molecular Formula |
C26H23N3O5
|
|---|---|
| Molecular Weight |
457.48
|
| CAS # |
2247240-76-0
|
| SMILES |
O1C=CC(C2CCC(CC12)OCC(NC1C=CC=C(C=1)NC(C1C=CC(=CC=1)N(C)C)=O)=O)=O
|
| 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)
|
| Solubility (In Vitro) |
DMSO : 83.33 mg/mL (182.15 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
