2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  3. ROCK
  4. CAY10746

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).

For research use only. We do not sell to patients.

CAY10746 Chemical Structure

CAY10746 Chemical Structure

CAS No. : 2247240-76-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 151 In-stock
Solution
10 mM * 1 mL in DMSO USD 151 In-stock
Solid
1 mg USD 60 In-stock
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 550 In-stock
50 mg USD 850 In-stock
100 mg USD 1350 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

CAY10746 Related Antibodies

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ROCK ROCK1 ROCK2

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Description

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)[1].

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.

CAY10746 Related Antibodies

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 0.1, 1 and 10 μM; 10 μM
Incubation Time: 2 h; 0.25, 1, 2 and 4 h
Result: Inhibited the phosphorylation of MYPT1 but did not impact the MYPT1 expression in dose-dependence and time- dependence.

Cell Proliferation Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 1 μM
Incubation Time: 5 days
Result: Significantly protected the cells from death.

Cell Migration Assay [1]

Cell Line: HUVEC cells
Concentration: 1 μM
Incubation Time: 24 h, 36 h
Result: Significantly reduced migrating cell numbers and significantly reduce the rate of wound healing at 24 h and 36 h.

Apoptosis Analysis[1]

Cell Line: ex vivo DR model
Concentration: 1 μM
Incubation Time: 5 days
Result: Significantly protected neuronal cells from death.
Molecular Weight

457.48

Formula

C26H23N3O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C=COC2=CC(OCC(NC3=CC(NC(C4=CC=C(N(C)C)C=C4)=O)=CC=C3)=O)=CC=C12
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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CAY10746 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CAY107462247240-76-0CAY 10746CAY-10746ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKdiabetic retinopathy (DR)Rho kinase (ROCK)ROCK IROCK IIInhibitorinhibitorinhibit

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