BIOLIMUS A9

中文名称:

BIOLIMUS A9

中文同义词:

42-O-(2-乙氧基乙基)雷帕霉素

英文名称:

UMiroliMus

英文同义词:

BioliMus;BioliMus, BioliMus A9, TRM 986;BIOLIMUS A9;UMiroliMus;Rapamycin, 42-O-(2-ethoxyethyl)-;BioliMus A9 UMiroliMus

CAS号:

851536-75-9

分子式:

C55H87NO14

分子量:

986.28

EINECS号:

相关类别:

微生物代谢物;Immunosuppressant;API

Mol文件:

851536-75-9.mol

沸点 

991.0±75.0 °C(Predicted)

密度 

1.15±0.1 g/cm3(Predicted)

酸度系数(pKa)

10.40±0.70(Predicted)

CAS 数据库

851536-75-9

生物活性

Umirolimus 是一种大环三烯内酯 Rapamycin 的衍生物，是一种强大的免疫抑制剂和抗炎剂。Umirolimus 具有高度的亲脂性，可用做药物洗脱支架。

体外研究

Umirolimus is a macrocyclic triene lactone, developed with pharmacological properties specifically tailored for localized drug delivery. Umirolimus can be used drug-eluting stent (DES) applications. Owing to its enhanced lipophilicity,it is strongly attracted to binding sites within the vessel wall and small, tortuous vessels, and contributing to cellular absorption and sustained distribution in the vessel wall surrounding the stent. Umirolimus prevents progression of the cell cycle in G1 phase by inhibiting IL-2/mTOR-mediated P70-KD S6 protein kinase activation. Umirolimus inhibits T-cell growth, as well as smooth muscle cell growth.

体内研究

The elimination half-life of Umirolimus is approximately 25 h in whole blood.