Rapamycin
Rapamycin is a macrolide initially produced by Streptomyces that exhibits immunosuppressive and pro-fibrotic activities. Rapamycin inhibits mTOR by binding FKBP12 and forming a complex that binds directly to mTOR; it is clinically used to prevent rejection in organ transplant patients. Rapamycin prevents IL-2-induced activation of T cells and B cells. Rapamycin also prevents IgA nephropathy, decreasing IgA deposition, inhibiting cell proliferation, and suppressing expression of α-SMA, type III collagen, PDGF, and TGF-β1. Additionally, rapamycin increases connective tissue growth factor levels in epithelial cells.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18957574
| Cas No. |
53123-88-9 |
|---|---|
| Purity |
≥98% |
| Formula |
C51H79NO13 |
| Formula Wt. |
914.17 |
| Synonym |
Sirolimus; Rapamune; AY-22989 |
| Melting Point |
183-185°C |
| Solubility |
Soluble in ether, chloroform, acetone, methanol, DMF, DMSO (20 mg/mL), and ethanol (up to 2 mM). Sparingly soluble in hexane and petr ether. Insoluble in water. |
| Appearance |
White Crystal Powder |
Klintmalm GB, Nashan B. The Role of mTOR Inhibitors in Liver Transplantation: Reviewing the Evidence. J Transplant. 2014;2014:845438. PMID: 24719752.
Tian J, Wang Y, Zhou X, et al. Rapamycin slows IgA nephropathy progression in the rat. Am J Nephrol. 2014;39(3):218-29. PMID: 24603476.
Xu X, Wan X, Geng J, et al. Rapamycin regulates connective tissue growth factor expression of lung epithelial cells via phosphoinositide 3-kinase. Exp Biol Med (Maywood). 2013 Sep;238(9):1082-94. PMID: 23986222.
