1. Epigenetics TGF-beta/Smad Cytoskeleton Cell Cycle/DNA Damage Stem Cell/Wnt
  2. PKC ROCK
  3. AR-13503

AR-13503  (Synonyms: AR-13324 M1 metabolite)

Cat. No.: HY-12798C Purity: 98.21%
Handling Instructions Technical Support

AR-13503 (AR-13324 M1 metabolite) is the hydrolytic metabolite of AR-13324 mesylate. AR-13324 is a ROCK kinase and PKC inhibitor with anti-angiogenic and retinal health-improving effects, showing potential for use in retinal disease research.

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

AR-13503 Chemical Structure

AR-13503 Chemical Structure

CAS No. : 2309668-15-1

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AR-13503 (AR-13324 M1 metabolite) is the hydrolytic metabolite of AR-13324 mesylate. AR-13324 is a ROCK kinase and PKC inhibitor with anti-angiogenic and retinal health-improving effects, showing potential for use in retinal disease research[1][2][3].

In Vitro

AR-13503 inhibits HUVEC angiogenesis in a dose-dependent manner (IC50 of 21 nM) and mouse choroidal angiogenesis[1].
AR-13503 enhances the barrier function of primary porcine retinal pigment epithelium (RPE) cells in a dose-dependent manner[1].
AR-13503 (1 mM to 0.5 μM) reduces axon retraction of rod photoreceptors during retinal detachment[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AR-13503 (1.25 mg/kg, i.p., once daily for 5 days) demonstrates significant inhibition of neovascularization in the oxygen-induced retinopathy mouse model[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Oxygen-induced retinopathy (OIR) mouse model (C57BL/6, 7 days old)[1]
Dosage: 1.25 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 5 days
Result: Detected in mouse retinas.
Reduced NV by ~55% compared to vehicle control when used with aflibercept.
Reduced NV by ~75% when used in combination with aflibercept.
Showed no significant differences in avascular areas among groups.
Molecular Weight

321.38

Formula

C19H19N3O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OCC1=CC=C([C@@H](CN)C(NC2=CC(C=CN=C3)=C3C=C2)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (124.46 mM; ultrasonic and adjust pH to 3 with HCl; 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 3.1116 mL 15.5579 mL 31.1158 mL
5 mM 0.6223 mL 3.1116 mL 6.2232 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 2.5 mg/mL (7.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

Purity: 98.21%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1116 mL 15.5579 mL 31.1158 mL 77.7895 mL
5 mM 0.6223 mL 3.1116 mL 6.2232 mL 15.5579 mL
10 mM 0.3112 mL 1.5558 mL 3.1116 mL 7.7790 mL
15 mM 0.2074 mL 1.0372 mL 2.0744 mL 5.1860 mL
20 mM 0.1556 mL 0.7779 mL 1.5558 mL 3.8895 mL
25 mM 0.1245 mL 0.6223 mL 1.2446 mL 3.1116 mL
30 mM 0.1037 mL 0.5186 mL 1.0372 mL 2.5930 mL
40 mM 0.0778 mL 0.3889 mL 0.7779 mL 1.9447 mL
50 mM 0.0622 mL 0.3112 mL 0.6223 mL 1.5558 mL
60 mM 0.0519 mL 0.2593 mL 0.5186 mL 1.2965 mL
80 mM 0.0389 mL 0.1945 mL 0.3889 mL 0.9724 mL
100 mM 0.0311 mL 0.1556 mL 0.3112 mL 0.7779 mL
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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.

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AR-13503
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