| CAS NO: | 99754-06-0 |
| 包装: | 100mg |
| 市场价: | 4032元 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 371.9 |
| Cas No. | 99754-06-0 |
| Formula | C21H22ClNO3 |
| Solubility | ≤33mg/ml in DMSO;33mg/ml in dimethyl formamide |
| Chemical Name | 4-chloro-2-[[(2E)-1-oxo-3-(4-pentylphenyl)-2-propen-1-yl]amino]-benzoic acid |
| Canonical SMILES | ClC1=CC(NC(/C=C/C2=CC=C(CCCCC)C=C2)=O)=C(C(O)=O)C=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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).
m.cnreagent.com