99754-06-0

ONO-RS-082 (99754-06-0) is a reversible inhibitor of Ca2+-independent phospholipase A2?(PLA2), IC50=7 μM for guinea pig lung PLA2.1?Inhibits epinephrine-induced thromboxane production in platelets.1?Inhibition of PLA2?by ONO-RS-032 disrupts endosome tubule formation and maintenance of the Golgi complex.2-4?Prevents Xenopus oocyte maturation at stage V.5

ONO-RS-082 is a potent PLA2 and epinephrine inhibitor.ONO-RS-082 is a phospholipase inhibitor.

previous study found that human platelets stimulated by epinephrine led to enhanced turnover of phosphatidylinositol 4,5-bisphosphate, accumulated inositol trisphosphate, diacylglycerol, and phosphatidic acid, indicating stimulation of phospholipase c. it was shown that these responses could be completely blocked by inhibitors of alpha 2-adrenergic receptors including ono-rs-082 or removal of fibrinogen. in addition, epinephrine could evoked an increased turnover of ester-linked arachidonic acid in aspirin treated platelets that was inhibited by ono-rs-082 or the absence of fibrinogen. moreover, it was found that ono-rs-082 at 3.5 μm was able to inhibit epinephrine-stimulated thromboxane production in human platelets. ono-rs-082 could also disrupt endosome tubule formation and maintenance of the golgi complex [1].

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1) Banga?et al.?(1986),?Activation of phospholipases A and C in human platelets exposed to epinephrine: role of glycoproteins IIb/IIIa and dual role of epinephrine; Proc. Natl. Acad. Sci. USA?83?9197 2) De Figueiredo?et al. (2001),?Inhibition of transferrin recycling and endosome tubulation by phospholipase A2 antagonists; J. Biol. Chem.?276?47361 3) Schmidt?et al. (2010),?A role for phospholipase A2 activity in membrane tubule formation and TGN trafficking; Traffic?11?1530 4) Bechler and Brown (2014),?Gβ1γ2 activates phospholipase A2-dependent Golgi membrane tubule formation; Front. Cell. Dev. Biol.?28?0004 5) Islam?et al.?(2005),?The distinct stage-specific effects of 2-(p-amylcinnamoyl)amino-4-chlorobenzoic acid on the activation of MAP kinase and Cdc2 kinase in Xenopus oocyte maturation; Cell Signal.?17?507