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BIOLOGICAL INFO
Solubility:
DMSO: 20mg/mL; H2O: <1mg/mL; EtOH: 4mg/mL
Application(s):
Specific Mammalian target of Rapamycin (mTOR) inhibitor
Form:
Free Base
REVIEW An immunosuppressant drug used to prevent rejection in organ transplantation. Sirolimus inhibits the response to interleukin-2 (IL-2), and thereby blocks activation of T and B cells. In contrast, tacrolimus inhibits the secretion of IL-2. The mode of action of sirolimus is to bind the cytosolic protein FK-binding protein 12 (FKBP12) in a manner similar to tacrolimus. Unlike the tacrolimus-FKBP12 complex which inhibits calcineurin (PP2B), though, the sirolimus-FKBP12 complex inhibits the mammalian target of rapamycin (mTOR) pathway by directly binding the mTOR Complex1 (mTORC1).
REFERENCES
[1]
Pagano, Thomas G.; Magnetic Resonance in Chemistry 2005, V43(2), P174-175; (2) Ley, Steven V.; Chemistry--A European Journal 2009, V15(12), P2874-2914.
[2]
V?zina C, Kudelski A, Sehgal SN (October 1975). Rapamycin (AY-22,989), a new antifungal antibiotic. J. Antibiot. 28 (10): 721u20136. PMID 1102508.
[3]
Pritchard DI (2005). Sourcing a chemical succession for cyclosporin from parasites and human pathogens. Drug Discovery Today 10 (10): 688-691. doi:10.1016/S1359-6446(05)03395-7. PMID 15896681.
[4]
McAlister VC, Mahalati K, Peltekian KM, Fraser A, MacDonald AS. (June 2002). A clinical pharmacokinetic study of tacrolimus and sirolimus combination immunosuppression comparing simultaneous to separated administration.. Ther Drug Monit. 24 (3): 346-50. PMID 12021624.
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