| Identification | Back Directory | [Name]
CAY10590 | [CAS]
1101136-50-8 | [Synonyms]
CAY10590
ANTPELWBOPVWPH-LJQANCHMSA-N
4-[(1-Oxo-7-phenylheptyl)amino]-(4R)-octanoic acid
Octanoic acid, 4-[(1-oxo-7-phenylheptyl)amino]-, (4R)- | [Molecular Formula]
C21H33NO3 | [MDL Number]
MFCD18382098 | [MOL File]
1101136-50-8.mol | [Molecular Weight]
347.49 |
| Chemical Properties | Back Directory | [Melting point ]
73-75 °C(Solv: ethyl acetate (141-78-6); ligroine (8032-32-4)) | [Boiling point ]
567.8±43.0 °C(Predicted) | [density ]
1.028±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 25 mg/ml; DMSO: 20 mg/ml; Ethanol: 30 mg/ml | [form ]
A crystalline solid | [pka]
4.60±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, liberating arachidonic acid for subsequent eicosanoid synthesis.1 Three primary types of PLA2 exist: secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2).2 Of these three enzymes, cPLA2 is the rate-limiting stimulus for release of arachidonic acid whereas sPLA2 amplifies the action of cPLA2 and regulates phagocytosis and foam cell formation.3 CAY10590, a simple amide based on (R)-γ-norleucine, is a potent and selective inhibitor of sPLA2. It exhibits 95% inhibition (XI(50) = 0.003) of sPLA2 at 0.091 mole fraction without affecting the activities of cPLA2 or iPLA2.4 | [Uses]
CAY10590 (GK115) is an inhibitor of secreted phospholipase A2 (sPLA2) and can be used for the research of chronic inflammatory kidney diseases[1]. | [IC 50]
sPLA2 | [References]
1. Dennis, E.A. Phospholipases The Enzymes XVI,(1983).
2. Dennis, E.A. Diversity of group types, regulation, and function of phospholipase A2 J. Biol. Chem. 269,13057-13060(1994).
3. Balestrieri, B., and Arm, J.P. Group V sPLA2: Classical and novel functions Biochim. Biophys. Acta 1761,1280-1288(2006).
4. Antonopoulou, G., Barbayianni, E., Magrioti, V., et al. Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A2 enzymes Bioorg. Med. Chem. 16,10257-10269(2008). |
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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 |
|