AR-13503
Based on 1 Customer Validation
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.21%
- No. CAS: 2309668-15-1
- Fòrmula: C19H19N3O2
- Peso molecular:321.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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
Actividad biológica
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Oxygen-induced retinopathy (OIR) mouse model (C57BL/6, 7 days old)[1]
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Dosage:1.25 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 5 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2309668-15-1
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Appearance Solid
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Peso molecular 321.38
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Fòrmula C19H19N3O2
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Color Off-white to light yellow
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SMILES
OCC1=CC=C([C@@H](CN)C(NC2=CC(C=CN=C3)=C3C=C2)=O)C=C1
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Synonyms
AR-13324 M1 metabolite
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 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.
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.
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 (272 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, 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 |
AR-13503 Related Classifications
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