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148554-65-8

中文名稱 利拉利汀
CAS 148554-65-8
分子式 C51H78NO13.Na
分子量 936.161
MOL 文件 148554-65-8.mol
更新日期 2023/03/20 15:41:25
148554-65-8 結(jié)構(gòu)式 148554-65-8 結(jié)構(gòu)式

基本信息

英文別名
SECO RAPAMYCIN SODIUM SALT
seco Rapamycin Sodium Salt, >85% By HPLC

物理化學(xué)性質(zhì)

熔點(diǎn)120-122°C
儲(chǔ)存條件Amber Vial, -20°C Freezer, Under Inert Atmosphere

常見問題列表

生物活性
Seco Rapamycin sodium salt 是 Rapamycin 的開環(huán)代謝物。Seco-Rapamycin 幾乎不影響 mTOR 功能。
體外研究

Disposition of Seco Rapamycin in Human Tissue Homogenates and Caco-2 Cell Monolayers. To determine whether Seco Rapamycin (D2) can be metabolized to dihydro Sirolimus (M2), 20 μM Seco Rapamycin is incubated with human liver, jejunal mucosal, and Caco-2 homogenates. All of these homogenates produced M2 in an NADPH-dependent manner. Ketoconazole, at a high concentration (100 μM), has no effect on the formation of M2 in any of the homogenates examined. To determine whether Seco Rapamycin can be metabolized to M2 in intact cells, 20 μM Seco Rapamycin is added to Caco-2 cell monolayers. When applied to the apical compartment, little Seco Rapamycin is detected in the basolateral compartment and in the cellular fraction after 4 h. In addition, little M2 is detected. LY335979 has little effect on the distribution of Seco Rapamycin after an apical dose, although M2 became detectable in the apical compartment. In contrast, when Seco Rapamycin is applied to the basolateral compartment, both Seco Rapamycin and M2 are readily detected in the apical compartment; LY335679 decreases the flux of Seco Rapamycin to the apical compartment and increases the amount of M2 in both apical and basolateral compartments.

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