| Identification | Back Directory | [Name]
CAY10502 | [CAS]
888320-29-4 | [Synonyms]
CAY10502
CAY10502,CAY-10502
CAY10502 Exclusive
NXDZVUAKVFVDSL-UHFFFAOYSA-N | [Molecular Formula]
C30H37NO7 | [MDL Number]
MFCD12912313 | [MOL File]
888320-29-4.mol | [Molecular Weight]
523.62 |
| Chemical Properties | Back Directory | [Boiling point ]
693.6±55.0 °C(Predicted) | [density ]
1.17±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 20 mg/ml; DMF:PBS (pH 7.2)(1:1): 0.5 mg/ml; DMSO: 10 mg/ml | [form ]
A crystalline solid | [pka]
4.05±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Phospholipase A2 (PLA2) catalyzes the hydrolysis of phospholipids at the sn-2 position leading to the production of lysophospholipids and free fatty acids. Calcium-dependent cytosolic PLA2 (cPLA2α) is a 85 kDa enzyme that plays a key role in the arachidonic cascade and the inflammatory response associated with this metabolic pathway.1 CAY10502 is a potent inhibitor of calcium-dependent cytosolic PLA2α (cPLA2α) with an IC50 value of 4.3 nM for the purified enzyme from human platelets.2 It inhibits arachidonic acid mobilization from A23187-stimulated or TPA-stimulated human platelets with IC50 values of 570 and 0.9 nM, respectively.2 | [Uses]
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]. | [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. |
| [IC 50]
cPLA2α: 4.3 nM (IC50) | [References]
1. Schaloske, R.H., and Dennis, E.A. The phospholipase A2 superfamily and its group numbering system Biochim. Biophys. Acta 1761,1246-1259(2006).
2. Ludwig, J., Bovens, S., Brauch, C., et al. Design and synthesis of 1-indol-1-yl-propan-2-ones as inhibitors of human cytosolic phospholipase A2α J. Med. Chem. 49,2611-2620(2006). |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|