| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
cPLA2α 4.3 nM (IC50)
The primary target of CAY10502 is calcium-dependent cytosolic phospholipase A2 alpha (cPLA2α). cPLA2α is a key enzyme in the arachidonic acid cascade, responsible for the hydrolysis of membrane phospholipids to release arachidonic acid, which is subsequently metabolized into various pro-inflammatory eicosanoids. By selectively inhibiting this enzyme, CAY10502 effectively disrupts the inflammatory signaling pathway at its source. |
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| ln Vitro |
With an inhibitory concentration of 0.0009 μM for TPA and 0.57 μM for A23187, CAY10502 prevents human platelets from releasing arachidonic acid when these factors are activated [1]. Prostaglandin E2 (PGE2) and VEGF synthesis caused by normoxic and hypoxic conditions are inhibited by CAY10502 (5, 20, 50 nM; 12 hours; Müller cells) [2]. CAY10502 (0.1-100 nM; 24 hours) prevents rat retinal microvascular endothelial cells (RRMEC) from proliferating when exposed to VEGF [2]. The phospholipid pool's release of arachidonic acid (AA) is inhibited by CAY10502 (10 μM), which also prevents the ELF-EMF-induced increase in AA (one hour) and the ELF-EMF suppression of Cav3.2 channels [3].
In vitro, CAY10502 is a highly potent inhibitor of purified human cPLA2α, with an IC50 of 4.3 nM. It effectively blocks arachidonic acid mobilization in human platelets stimulated by A23187 and TPA, with IC50 values of 570 nM and 0.9 nM, respectively. In Müller cells, CAY10502 (5, 20, 50 nM) inhibits hypoxia-induced production of prostaglandin E2 (PGE2) and VEGF. Furthermore, it suppresses VEGF-induced proliferation of rat retinal microvascular endothelial cells (RRMEC) in a concentration-dependent manner (0.1-100 nM). |
| ln Vivo |
Rats with oxygen-induced retinopathy (OIR) showed a dose-dependent inhibitory impact on retinal neovascularization (NV) in the eyes injected with CAY10502 (2.5, 25, 100 nM; 5 μL)[2].
In vivo, CAY10502 has demonstrated efficacy in a rat model of oxygen-induced retinopathy (OIR). Intravitreal injection of CAY10502 (2.5, 25, 100 nM; 5 μL) resulted in a dose-dependent inhibition of retinal neovascularization (NV). At the highest dose of 100 nM, a 53.1% reduction in retinal NV was observed. This in vivo efficacy supports its potential as a research tool for studying diseases involving pathological angiogenesis and inflammation. |
| Enzyme Assay |
The in vitro enzyme activity of CAY10502 is typically assessed using purified human cPLA2α enzyme. The assay involves incubating the enzyme with a radiolabeled or fluorescent phospholipid substrate in the presence of varying concentrations of the inhibitor. The hydrolysis of the substrate, which releases arachidonic acid or a labeled product, is measured, and the IC50 value is determined from the concentration-response curve.
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: RRMEC Tested Concentrations: 0.1-100 nM Incubation Duration: 24 hrs (hours) Experimental Results: CAY10502 (35, 50 nM) demonstrated significant reductions in VEGF-induced proliferation (64.3% and 84.1%, respectively) compared with cultures treated with VEGF alone. In vitro cellular assays for CAY10502 often use human platelets or retinal cell lines. For platelet assays, cells are pre-incubated with the compound and then stimulated with agents like A23187 or TPA to trigger arachidonic acid release, which is subsequently measured. In retinal research, Müller cells or retinal microvascular endothelial cells are treated with CAY10502, and the inhibition of VEGF-induced proliferation or hypoxia-induced PGE2 and VEGF production is quantified. |
| Animal Protocol |
Animal/Disease Models: OIR and room air (RA) SD (Sprague-Dawley) rat[2]
Doses: 2.5, 25, 100 nM; 5 μL Route of Administration: Intravitreal Injection Experimental Results: Injection of 100 nM CAY10502 resulted in a 53.1% reduction in NV compared with vehicle treatment. In vivo studies for CAY10502 have been conducted in a rat model of oxygen-induced retinopathy (OIR). The compound is administered via intravitreal injection at doses such as 2.5, 25, and 100 nM in a 5 μL volume. The primary endpoint is the quantification of retinal neovascularization, which is assessed and compared to control groups to determine the compound's inhibitory efficacy. |
| ADME/Pharmacokinetics |
CAY10502 is a small molecule with a molecular weight of 523.62 g/mol. It is soluble in DMSO at a concentration of 12.5 mg/mL (23.87 mM) with ultrasonic and warming. For research purposes, the powder can be stored at -20°C for up to 3 years, and solutions can be stored at -80°C for up to 6 months. Detailed ADME parameters such as half-life and bioavailability are not publicly available.
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| Toxicity/Toxicokinetics |
Specific toxicity data for CAY10502 is not extensively detailed in the provided literature. As a research chemical, it is intended for laboratory use only and should be handled with standard safety precautions. It is not approved for human therapeutic use.
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| References |
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| Additional Infomation |
CAY10502 is a potent cPLA2α inhibitor used to study the role of the arachidonic acid cascade in inflammation and pathological angiogenesis, particularly in models of retinopathy. Its high potency (IC50 = 4.3 nM) and in vivo efficacy in reducing retinal neovascularization make it a valuable tool for investigating diseases like diabetic retinopathy and age-related macular degeneration. The compound is available from various chemical suppliers for research purposes.
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| Molecular Formula |
C30H37NO7
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|---|---|
| Molecular Weight |
523.62
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| Exact Mass |
523.257
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| CAS # |
888320-29-4
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| PubChem CID |
11670893
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
693.6±55.0 °C at 760 mmHg
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| Flash Point |
373.3±31.5 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.559
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| LogP |
7.96
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
38
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| Complexity |
736
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCCCOC1=CC=C(C=C1)OCC(=O)CN2C=C(C3=C2C=CC(=C3)C(=O)O)C(=O)OC
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| InChi Key |
NXDZVUAKVFVDSL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H37NO7/c1-3-4-5-6-7-8-9-10-17-37-24-12-14-25(15-13-24)38-21-23(32)19-31-20-27(30(35)36-2)26-18-22(29(33)34)11-16-28(26)31/h11-16,18,20H,3-10,17,19,21H2,1-2H3,(H,33,34)
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| Chemical Name |
1-[3-(4-decoxyphenoxy)-2-oxopropyl]-3-methoxycarbonylindole-5-carboxylic acid
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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: 12.5 mg/mL (23.87 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9098 mL | 9.5489 mL | 19.0978 mL | |
| 5 mM | 0.3820 mL | 1.9098 mL | 3.8196 mL | |
| 10 mM | 0.1910 mL | 0.9549 mL | 1.9098 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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