Indomethacin farnesil

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CAS NO:

85801-02-1

Indometacin farnesil

Indomethacin farnesil 是具有口服活性的、Indomethacin 的前体药物。Indomethacin (Indometacin) 是一种有效的，可透过血脑屏障的，非选择性的COX1和COX2抑制剂，在 CHO 细胞中，对人 COX-1 和 COX-2 的IC₅₀值分别为 18 nM 和 26 nM。Indomethacin 通过干扰溶酶体的正常功能来破坏自噬流 (autophagic flux)。

生物活性

Indomethacin farnesil is an orally active prodrug of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor ofCOX1andCOX2, withIC₅₀sof 18 nM and 26 nM for humanCOX-1andCOX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes^[1]^[2].

体外研究
(In Vitro)

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^[2].

体内研究
(In Vivo)

Indomethacin farnesil (IMF) can effectively release indomethacin when administered locally^[1].

Animal Model:	Rats^[1].
Dosage:	50 nmol a rat paw.
Administration:	Once.
Result:	Reduced the level of PGE₂in a dose dependent manner.

分子量

562.14

Formula

C₃₄H₄₀ClNO₄

CAS 号

85801-02-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.