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

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

Cat. No.: HY-125639 Purity: 98.01%
SDS COA Handling Instructions Technical Support

(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice.

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

(rac)-AR-13503 Chemical Structure

(rac)-AR-13503 Chemical Structure

CAS No. : 1254032-16-0

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Based on 1 publication(s) in Google Scholar

Other Forms of (rac)-AR-13503:

(rac)-AR-13503 Related Antibodies

Top Publications Citing Use of Products

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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ROCK ROCK1 ROCK2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice[1][2].

In Vitro

AR-13503 (16 h) inhibits human umbilical vein endothelial cell (HUVEC) tube formation, with an IC50 value of 21 nM[1].
AR-13503 (400 nM; 5 d) decreases the sprouting area of the choroidal in a dose-dependent manner[1].
AR-13503 (400 nM; 2 weeks) enhances primary porcine RPE barrier function in a dose-dependent manner[1].

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

(rac)-AR-13503 Related Antibodies
In Vivo

AR-13503 (1.25 mg/kg; i.p.; once daily for 5 days) in collaboration with Aflibercept (HY-108801), significantly decreases the development of aberrant neovascularization (NV)[1].

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

Animal Model: Oxygen-induced retinopathy (OIR) mice model (C57BL/6; 7-days-old)[1]
Dosage: 1.25 mg/kg
Administration: Intraperitoneal injection; once daily for 5 days
Result: The combination group had a greater (~75%) reduction in NV than Aflibercept alone (~55%).
Clinical Trial
Molecular Weight

321.37

Formula

C19H19N3O2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C(CN)C1=CC=C(CO)C=C1)NC2=CC3=C(C=C2)C=NC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (124.47 mM; ultrasonic and warming and adjust pH to 2 with 1 M HCL 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 3.1117 mL 15.5584 mL 31.1168 mL
5 mM 0.6223 mL 3.1117 mL 6.2234 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 (protect from light). 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
=
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: ≥ 4 mg/mL (12.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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: ≥ 4 mg/mL (12.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 (protect from light). 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 3.1117 mL 15.5584 mL 31.1168 mL 77.7920 mL
5 mM 0.6223 mL 3.1117 mL 6.2234 mL 15.5584 mL
10 mM 0.3112 mL 1.5558 mL 3.1117 mL 7.7792 mL
15 mM 0.2074 mL 1.0372 mL 2.0745 mL 5.1861 mL
20 mM 0.1556 mL 0.7779 mL 1.5558 mL 3.8896 mL
25 mM 0.1245 mL 0.6223 mL 1.2447 mL 3.1117 mL
30 mM 0.1037 mL 0.5186 mL 1.0372 mL 2.5931 mL
40 mM 0.0778 mL 0.3890 mL 0.7779 mL 1.9448 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 0.3890 mL 0.9724 mL
100 mM 0.0311 mL 0.1556 mL 0.3112 mL 0.7779 mL
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(rac)-AR-13503 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:

(rac)-AR-135031254032-16-0(rac)-AR-13324 M1 metabolitePKCROCKProtein kinase CRho-associated protein kinaseRho-associated kinaseRho-kinaseROKInhibitorinhibitorinhibit

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