| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
AR-13503 is a metabolite of AR-13324, which targets two classes of enzymes: ROCK (Rho-associated protein kinase) and PKC (Protein Kinase C). Both are involved in regulating cell shape, movement, and survival. AR-13324, the parent compound, is a dual inhibitor of these pathways. AR-13503, as the hydrolysis metabolite, may retain some of this activity and is believed to contribute to the anti-angiogenic and retinal health-improving effects of the parent drug.
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| ln Vitro |
In vitro, AR-13503 is used to study the biological activity of the AR-13324 parent compound's metabolism. AR-13324, and presumably its active metabolite AR-13503, inhibit ROCK kinase and PKC activity. The anti-angiogenic properties can be studied using in vitro models such as the inhibition of endothelial cell tube formation on a Matrigel matrix, or the inhibition of HUVEC (Human Umbilical Vein Endothelial Cells) proliferation and migration.
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| ln Vivo |
In vivo, the effects of AR-13503 are expected to be similar to those of its parent compound, AR-13324. AR-13324 has been shown to have anti-angiogenic and retinal health-improving effects, making it a candidate for research into retinal diseases such as diabetic retinopathy, glaucoma, and age-related macular degeneration. As the active metabolite, AR-13503 likely contributes to these in vivo outcomes after administration of the parent drug.
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| Enzyme Assay |
AR-13503 can be used as a standard for enzyme kinetics studies. For example, it can be used to study the activity of hydrolytic enzymes (e.g., esterases) that convert AR-13324 mesylate to this metabolite. In a non-cellular assay, purified AR-13324 is incubated with microsomes or purified esterases, and the appearance of AR-13503 is quantified over time using HPLC or LC-MS with AR-13503 as an analytical reference standard.
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| Cell Assay |
AR-13503 is not typically used as a direct treatment in cell-based assays. Instead, it is used as an analytical standard to quantify the concentration of this active metabolite in cellular samples. For example, retinal pigment epithelial (RPE) cells (e.g., ARPE-19 cell line) are treated with AR-13324. At various time points, cell lysates and culture media are collected. AR-13503 is used as a standard to create a calibration curve for LC-MS analysis, allowing researchers to measure the amount of metabolite generated by the cells from the parent compound.
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| Animal Protocol |
For in vivo pharmacokinetic studies, AR-13503 is not administered directly but is measured as a metabolite in plasma or tissue samples. Animals (typically rats or mice) are dosed with AR-13324 mesylate (e.g., via oral gavage or intravenous injection). Blood samples are collected at multiple time points, and the plasma is analyzed. Using AR-13503 as a reference standard in LC-MS analysis, the concentration-time profile of this metabolite is determined. This provides critical data on the rate of formation and elimination of the active metabolite.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic (PK) parameters for AR-13503 itself are derived from studies of its parent compound, AR-13324. The metabolite's appearance and elimination in the plasma will follow a specific PK profile, with parameters such as Tmax (time to reach maximum concentration), Cmax (maximum concentration), and terminal half-life (t1/2) being calculated from its concentration-time curve. These parameters are crucial for understanding the compound's in vivo behavior.
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| Toxicity/Toxicokinetics |
Specific toxicological data for AR-13503 is not extensively published, as it is primarily an analytical standard for a research compound. The safety profile is expected to be similar to that of the parent compound, AR-13324. Standard laboratory safety precautions for handling research-use metabolites should be observed, including the use of personal protective equipment (PPE) such as gloves, lab coats, and safety glasses.
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| Additional Infomation |
AR-13503 is not an approved drug. It is a research-use metabolite standard and an analytical reference compound. It is used in the research of retinal diseases such as diabetic retinopathy, glaucoma, and age-related macular degeneration (AMD). Its value lies in being able to accurately identify and quantify the active form of a potential therapeutic agent in preclinical studies, which is a critical step in drug development.
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| Molecular Formula |
C19H19N3O2
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|---|---|
| Molecular Weight |
321.37
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| Exact Mass |
321.147
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| CAS # |
2309668-15-1
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| PubChem CID |
134128281
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.310±0.06 g/cm3(Predicted)
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| Boiling Point |
649.2±55.0 °C(Predicted)
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
409
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC(=CC=C1CO)[C@@H](CN)C(=O)NC2=CC3=C(C=C2)C=NC=C3
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| InChi Key |
LTXBFJFJUIJOQE-GOSISDBHSA-N
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| InChi Code |
InChI=1S/C19H19N3O2/c20-10-18(14-3-1-13(12-23)2-4-14)19(24)22-17-6-5-16-11-21-8-7-15(16)9-17/h1-9,11,18,23H,10,12,20H2,(H,22,24)/t18-/m1/s1
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| Chemical Name |
(2S)-3-amino-2-[4-(hydroxymethyl)phenyl]-N-isoquinolin-6-ylpropanamide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 25 mg/mL (77.79 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.78 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 25.0 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: ≥ 2.5 mg/mL (7.78 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3112 mL | 1.5558 mL | 3.1117 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.
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