产品
编 号:F483285
分子式:C34H40ClNO4
分子量:562.14
产品类型
结构图
CAS No: 85801-02-1
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产品详情
生物活性:
Indomethacin farnesil is an orally active proagent of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
体内研究:
Indomethacin farnesil (IMF) can effectively release indomethacin when administered locally.Animal Model:Rats.
Dosage:50 nmol a rat paw.
Administration:Once.
Result:Reduced the level of PGE2 in a dose dependent manner.
体外研究:
Indometacin farnesil (IMF) is a newly synthesized prodrug of indomethacin designed to reduce the occurrence of side-effects by esterification of the carboxyl group of indomethacin with farnesol. This modification is intended to decrease the extraction and subsequent rapid metabolism of the drug by the liver, so that lymphatic absorption would become a major route, and it was also anticipates that hydrolytic enzymes present in plasma and tissues, including inflamed tissue, would release indomethacin effectively from IMF.