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888320-29-4

888320-29-4 structure
888320-29-4 structure
  • Name: CAY10502
  • Chemical Name: cay10502
  • CAS Number: 888320-29-4
  • Molecular Formula: C30H37NO7
  • Molecular Weight: 523.617
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
  • Create Date: 2017-03-26 14:59:15
  • Modify Date: 2024-01-22 18:04:33
  • 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].

Name cay10502
Synonyms 1H-Indole-3,5-dicarboxylic acid, 1-[3-[4-(decyloxy)phenoxy]-2-oxopropyl]-, 3-methyl ester
1-{3-[4-(Decyloxy)phenoxy]-2-oxopropyl}-3-(methoxycarbonyl)-1H-indole-5-carboxylic acid
Description 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].
Related Catalog
Target

cPLA2α:4.3 nM (IC50)

In Vitro 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: RRMEC Concentration: 0.1-100 nM Incubation Time: 24 hours Result: 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 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: OIR and room air (RA) Sprague-Dawley rat[2] Dosage: 2.5, 25, 100 nM; 5 μL Administration: Intravitreal Injection Result: Injection of 100 nM CAY10502 resulted in a 53.1% reduction in NV compared with vehicle treatment.
References

[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.

Density 1.2±0.1 g/cm3
Boiling Point 693.6±55.0 °C at 760 mmHg
Molecular Formula C30H37NO7
Molecular Weight 523.617
Flash Point 373.3±31.5 °C
Exact Mass 523.257019
PSA 104.06000
LogP 7.96
Vapour Pressure 0.0±2.3 mmHg at 25°C
Index of Refraction 1.559
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