| Bioactivity | CAY10502 is a potent, calcium-dependent cytosolic phospholipase A2 α (cPLA2α) inhibitor with an IC50 of 4.3 nM for isolated enzyme. CAY10502 can be used in the research of retinopathy and inflammatory diseases[1][2][3]. | |||||||||
| Invitro | CAY10502 inhibits the release of arachidonic acid mediated by cPLA2R stimulanted with A23187 and TPA in human platelets, with IC50s of 0.57 and 0.0009 μM, respectively[1].CAY10502 (5, 20, 50 nM; 12 hours; müller cells) inhibits normoxic- and hypoxia-induced Prostaglandin E2 (PGE2) and VEGF production[2].CAY10502 (0.1-100 nM; 24 hours) inhibits the VEGF-induced proliferation of rat retinal microvascular endothelial cells (RRMEC)[2].CAY10502 (10 μM) inhibits arachidonic acid (AA) release from the phospholipid pools, abrogated extremely low-frequency electromagnetic fields (ELF-EMF; 1 h) induced AA increase and the ELF-EMF inhibitory effect of Cav3.2 channels[3]. Cell Proliferation Assay[2] Cell Line: | |||||||||
| In Vivo | CAY10502-injected (2.5, 25, 100 nM; 5 μL) eyes demonstrates a dose-dependent inhibition of retinal neovascularization (NV) in rat oxygen-induced retinopathy (OIR)[2]. Animal Model: | |||||||||
| Name | CAY10502 | |||||||||
| CAS | 888320-29-4 | |||||||||
| Formula | C30H37NO7 | |||||||||
| Molar Mass | 523.62 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Pohjala L L, et al. Interference by bovine serum albumin in PED6 based phospholipase A2 screening assays[J]. Die Pharmazie, 2012. [2]. Barnett JM, et al. Role of cytosolic phospholipase A(2) in retinal neovascularization. Invest Ophthalmol Vis Sci. 2010;51(2):1136-1142. [3]. Cui Y, et al. 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. |