Seco Rapamycin ethyl ester 是 Rapamycin 的开环代谢物。Seco-Rapamycin 几乎不影响 mTOR 功能。

Seco Rapamycin ethyl ester is an open-ring metabolite of Rapamycin derivative. Seco-rapamycin is reported not to affect the mTOR function.

Oil

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), 20μM 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 (100μM), 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, 20μM 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 th

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

[1]. Paine MF, et al. Identification of a novel route of extraction of sirolimus in human small intestine: roles ofmetabolism and secretion. J Pharmacol Exp Ther. 2002 Apr;301(1):174-86.

In Vitro: DMSO : 100 mg/mL (106.13 mM; Need ultrasonic)配制储备液