Rapamycin-¹³C,d₃  (Synonyms: 雷帕霉素; 西罗莫司-¹³C,d₃; Sirolimus-¹³C,d₃; AY-22989-¹³C,d₃)

Rapamycin-¹³C,d₃ (Sirolimus-¹³C,d₃; AY-22989-¹³C,d₃) is the ¹³C and deuterium labeled Rapamycin (HY-10219)^[1].Rapamycin is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant^[1][2].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

918.18

C₅₀¹³CH₇₆D₃NO₁₃

53123-88-9

固体

White to off-white

雷帕霉素-¹³C,d₃；西罗莫司-¹³C,d₃

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]. Edwards SR, et al. The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem, 2007, 282(18), 13395-13401.  [Content Brief]

  [2]. Rangaraju S, et al. Rapamycin activates autophagy and improves myelination in explant cultures from neuropathicmice. J Neurosci. 2010 Aug 25;30(34):11388-97.  [Content Brief]