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851536-75-9

中文名稱 BIOLIMUS A9
英文名稱 UMiroliMus
CAS 851536-75-9
分子式 C55H87NO14
分子量 986.28
MOL 文件 851536-75-9.mol
851536-75-9 結(jié)構(gòu)式 851536-75-9 結(jié)構(gòu)式

基本信息

中文別名
42-O-(2-乙氧基乙基)雷帕霉素
英文別名
BioliMus
UMiroliMus
BIOLIMUS A9
BioliMus A9 UMiroliMus
BioliMus, BioliMus A9, TRM 986
Rapamycin, 42-O-(2-ethoxyethyl)-

物理化學(xué)性質(zhì)

沸點(diǎn)991.0±75.0 °C(Predicted)
密度1.15±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMF: Soluble; DMSO: Soluble; Ethanol: Soluble; Methanol: Soluble
酸度系數(shù)(pKa)10.40±0.70(Predicted)
形態(tài)固體
顏色White to light yellow

常見問題列表

生物活性
Umirolimus 是一種大環(huán)三烯內(nèi)酯 Rapamycin 的衍生物,是一種強(qiáng)大的免疫抑制劑和抗炎劑。Umirolimus 具有高度的親脂性,可用做藥物洗脫支架。
體外研究

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.

體內(nèi)研究

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

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