CAY10502 是一种有效的钙依赖性胞质磷脂酶 A2 α(cPLA2α) 抑制剂，对分离的酶具有IC50为 4.3 nM。CAY10502 可用于视网膜病变和炎症性疾病的研究。
| 生物活性 | CAY10502 is a potent, calcium-dependentcytosolicphospholipaseA2 α(cPLA2α) inhibitor with anIC50of 4.3 nM for isolated enzyme. CAY10502 can be used in the research of retinopathy and inflammatory diseases[1][2][3]. |
| IC50& Target[1] | |
体外研究
(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. |
|
体内研究
(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. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
m.cnreagent.com