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ONO-RS-082
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ONO-RS-082图片
CAS NO:99754-06-0
包装与价格:
包装价格(元)
25mg电议
100mg电议

产品介绍
ONO-RS-082 是一种磷脂酶 A (PLA) 的抑制剂。
Cas No.99754-06-0
化学名4-chloro-2-[[(2E)-1-oxo-3-(4-pentylphenyl)-2-propen-1-yl]amino]-benzoic acid
Canonical SMILESClC1=CC(NC(/C=C/C2=CC=C(CCCCC)C=C2)=O)=C(C(O)=O)C=C1
分子式C21H22ClNO3
分子量371.9
溶解度≤33mg/ml in DMSO;33mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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 [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Banga, H. S.,Simons, E.R.,Brass, L.F., et al. 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(23), 9197-9201 (1986).