产品名称

他克莫司(Tacrolimus)

一般描述

Tacrolimus(他克莫司) a macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis, is a Calcineurin Inhibitor Immunosuppressant.

别 称

Fujimycin; Prograf; Protopic;  Tsukubaenolide;FK-506

纯 度

≥99%(HPLC)

CAS NO.

104987-11-3

分子式

C⁴⁴H⁶⁹NO¹²

分子量

804.031

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色或类白色固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥50mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

Tacrolimus is a macrolide antibiotic. It acts by reducing peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This inhibits both T-lymphocyte signal transduction and IL-2 tranion.  Although this activity is similar to cyclosporine studies have shown that the incidence of acute rejection is reduced by tacrolimus use over cyclosporine. Tacrolimus has also been shown to be effective in the topical treatment of eczema, particularly atopic eczema. It suppresses inflammation in a similar way to steroids, but is not as powerful. An important dermatological advantage of tacrolimus is that it can be used directly on the face; topical steroids cannot be used on the face, as they thin the skin dramatically  there. On other parts of the body, topical steroid are generally a better treatment.

Anhydrous from of tacrolimus, a macrolide isolated from Streptomyces tsukubaensis. Tacrolimus binds to the FKBP-12  protein and forms a complex with calcium-dependent proteins, thereby inhibiting calcineurin phosphatase activity and resulting in decreased cytokine production. This agent exhibits potent immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation. Tacrolimus possesses similar immunosuppressive properties to cyclosporine, but is more potent.

l  包装与存储

包 装

25mg; 100mg

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.   https://www.ncbi.nlm.nih.gov