Olsalazine disodium,6054-98-4

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产品名称：Olsalazine disodium

产品别名：奥沙拉秦钠

英文别名：Olsalazine disodium

靶点：COX；IFγ

CAS：6054-98-4

纯度：＞98%

外观：黄色结晶性粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Olsalazine sodium is bioconverted to 5-aminosalicylic acid (5-ASA) in the colon and has anti-inflammatory activity in ulcerative colitis.

溶解性：DMSO : 4 mg/mL (11.55 mM)
Water : 38 mg/mL (109.8 mM)

体外研究：

Olsalazine displays multiple effects on intestinal electrolyte. In vitro application of Olsalazine (Olsalazine is potent inhibitors of human intestinal macrophages chemotaxis to LTB4 with IC50 of 0.39 mM. Olsalazine (0.4 mM) inhibits the superoxide radical production generated by phorbol myristate acetate (PMA)-activated neutrophils or by xanthine-xanthine oxidase reaction by reduction of 31% and 73%, respectively. Other suggested possible mechanisms by which Olsalazine-derived mesalazine might ameliorate colonic mucosa/inflammation are inhibition of platelet activating factor, inhibition of cytokine production in human mononuclear cells, suppression of colonic fatty acid oxidation, inhibition of endothelial cell proliferation by folic acid antagonism, inhibition of leukotriene synthesis from arachidonic acid via inhibition of lipoxygenase, modulation of the prostaglandin profile by an effect on prostaglandin 15-hydroxydehydrogenase, and interference with leukocyte function.

体内研究：Olsalazine is developed as a way of delivering mesalazine to the colon, since very little of parent molecule is absorbed from the gastrointestinal tract following oral administration. In the colon, azoreductase bacteria cleave the azo bond, releasing 2 molecules of mesalazine which has demonstrated therapeutic effect in inflammatory bowel diseases. Olsalazine (50mg/kg/day) significantly prolongs the survival of nu/nu CD-1 mice with experimental colitis induced by dextran sulphate sodium. Olsalazine inhibits tumor growth in a rodent model of colorectal cancer. In 1,2-dimethylhydrazine-treated rats, Olsalazine (25 mg/kg/day) decreases number and volume of tumors by 58.17% and 62.67%, respectively. Administration of Olsalazine induces a 1.7-fold times increase in the number of apoptotic cells, companied with a reduction of 42.4% in cell proliferation rate.

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