CAY10502 is a potent calcium-dependent cytosolic phospholipase A2 alpha (cPLA2α) inhibitor (antagonist) with IC50 of 4.3 nM against the isolated enzyme. CAY10502 may be utilized to study retinopathy and inflammatory diseases.

Physicochemical Properties

Molecular Formula	C30H37NO7
Molecular Weight	523.62
Exact Mass	523.257
CAS #	888320-29-4
PubChem CID	11670893
Appearance	White to off-white solid powder
Density	1.2±0.1 g/cm3
Boiling Point	693.6±55.0 °C at 760 mmHg
Flash Point	373.3±31.5 °C
Vapour Pressure	0.0±2.3 mmHg at 25°C
Index of Refraction	1.559
LogP	7.96
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	18
Heavy Atom Count	38
Complexity	736
Defined Atom Stereocenter Count	0
InChi Key	NXDZVUAKVFVDSL-UHFFFAOYSA-N
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)
Chemical Name	1-[3-(4-decoxyphenoxy)-2-oxopropyl]-3-methoxycarbonylindole-5-carboxylic acid
HS Tariff Code	2934.99.9001
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)

Biological Activity

Targets	cPLA2α 4.3 nM (IC50)
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].
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].
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.
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.
References	[1]. Interference by bovine serum albumin in PED6 based phospholipase A2 screening assays. Die Pharmazie, 2012. [2]. Role of cytosolic phospholipase A(2) in retinal neovascularization. Invest Ophthalmol Vis Sci. 2010;51(2):1136-1142. [3]. Exposure to extremely low-frequency electromagnetic fields inhibits T-type calcium channels via AA/LTE4 signaling pathway. Cell Calcium. 2014 Jan;55(1):48-58.

Solubility Data

Solubility (In Vitro)

DMSO: 12.5 mg/mL (23.87 mM)

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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (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.