Description
ONO-RS-082 is a reversible inhibitor of Ca2+-independent phospholipase A2. Phospholipases A2 (PLA2s) are enzymes releasing fatty acids from the second carbon group of glycerol. This particular phospholipase can specifically recognize the sn-2 acyl bond of phospholipids and can catalytically hydrolyze the bond releasing arachidonic acid and lysophosphatidic acid.. In vitro: 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 . In vivo: Up to now, there is no animal in vivo data reported. Clinical trial: So far, no clinical study has been conducted.
Product information
CAS Number: 99754-06-0
Molecular Weight: 371.86
Formula: C21H22ClNO3
Chemical Name: 4-chloro-2-[(2E)-3-(4-pentylphenyl)prop-2-enamido]benzoic acid
Smiles: CCCCCC1C=CC(/C=C/C(=O)NC2C=C(Cl)C=CC=2C(O)=O)=CC=1
InChiKey: MDVFITMPFHDRBZ-JLHYYAGUSA-N
InChi: InChI=1S/C21H22ClNO3/c1-2-3-4-5-15-6-8-16(9-7-15)10-13-20(24)23-19-14-17(22)11-12-18(19)21(25)26/h6-14H,2-5H2,1H3,(H,23,24)(H,25,26)/b13-10+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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