13181  CAY10590

(CAS 1101136-50-8)

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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
1  Dennis, E.A. Phospholipases. Enzymes XVI, 307-353 (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., 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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This product is also available to buy in bulk quantities. Please contact our Sales Department for a quote or to purchase.

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Warning This product is not for human or veterinary use.

Pricing updated 2010-03-18.
Prices are subject to change without notice.

Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.

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