| Source: | Streptomyces
hygroscopicus subsp hygroscopicus
|
| Synonyms | RAPA, Rapamune, Sirolimus, RPM, Antibiotic AY 22989 |
| Description: | Rapamycin (Sirolimus) is a macrolide compound that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus (Rapamycin) is a potent immunosuppressant. Sirolimus (Rapamycin) possesses both antifungal and antineoplastic properties. |
| CAS number: | 53123-88-9 |
| Merck index: | 12, 8288 |
| Molecular weight: | 914.2 |
| Structure: | 
 |
| Molecular Formula: | C51H79NO13 |
| Canonical SMILES: |
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Solubility
information: | Methanol, DMSO |
| Specifications |
|
| Appearance: | Off-white to slight yellow powder |
| Purity: | At least 97% by TLC, HPLC |
| λmax: | 265, 277, 287 |
| Melting point | 178°C-182°C |
| Solubility | Rapamycin (Sirolimus) gives clear colorless solution at 50mg/ml DMSO |
| Storage | -20°C. Protect from light and moisture. Hygroscopic. |
| Applications | Medical applications: Rapamycin (Sirolimus) is an immunosuppressant and is used to prevent rejection of kidney and liver transplants. It is also used sometimes in cases of psoriasis, dermatitis. Research applications: Rapamycin Sirolimus inhibits cell motility by suppression of mTOR-mediated S6K1 and 4E-BP1 pathways. Rapamycin Sirolimus inhibits T-lymphocyte activation / proliferation occuring in response to antigenic and cytokine (Interleukin IL-2, IL-4, and IL-15) stimulation by a mechanism that is distinct from that of other immunosuppressing agents. Sirolimus also inhibits antibody production. |
| Warnings | MAY HARMFUL IF SWALLOWED |
| Classification | macrolide
immunosuppressor |
| Related products | |
| | For Research use only. Not for Human or Drug use
GMP/API grade available on request
Rapamycin by Fermentek is not produced from or contains any ingredients from animal origin.
No genetically modified organisms are used. |
| Publications | |
| | Ge L, Iakovou I, Cosgrave J, Chieffo A, Montorfano M, Michev I, Airoldi F, Carlino M, Melzi G, Sangiorgi GM, Corvaja N, Colombo A.
Immediate and mid-term outcomes of Sirolimus (Rapamycin) -eluting stent implantation for chronic total occlusions.
Eur Heart J. 2005 Apr 7 |
| | Kerkar N, Dugan C, Rumbo C, Morotti RA, Gondolesi G, Shneider BL, Emre S.
Sirolimus (Rapamycin) successfully treats post-transplant autoimmune hepatitis.
Am J Transplant. 2005 May;5(5):1085-9 |
| | Steiner D, Brunicki N, Bachar-Lustig E, Taylor PA, Blazar BR, Reisner Y.
Overcoming T cell-mediated rejection of bone marrow allografts by T-regulatory cells: Synergism with veto cells and rapamycin. (Sirolimus)
Exp Hematol. 2006 Jun;34(6):802-8 |
| | Liu Y.
Rapamycin and chronic kidney disease: beyond the inhibition of inflammation.
Kidney Int. 2006 Jun;69(11):1925-7. |
| | Okuno S.
Mammalian target of rapamycin inhibitors in sarcomas.
Curr Opin Oncol. 2006 Jul;18(4):360-2 |
| | Liu L, Li F, Cardelli JA, Martin KA, Blenis J, Huang S.
Rapamycin inhibits cell motility by suppression of mTOR-mediated S6K1 and 4E-BP1 pathways.
Oncogene. 2006 May 22 |
| | Aggarwal D, Fernandez ML, Soliman GA.
Rapamycin (Sirolimus), an mTOR inhibitor, disrupts triglyceride metabolism in guinea pigs.
Metabolism. 2006 Jun;55(6):794-802 |
| | Jiang X, Yeung RS.
Regulation of Microtubule-Dependent Protein Transport by the TSC2/Mammalian Target of Rapamycin Pathway.
Cancer Res. 2006 May 15;66(10):5258-69 |
| | Marderosian M, Sharma A, Funk AP, Vartanian R, Masri J, Jo OD, Gera JF.
Tristetraprolin regulates Cyclin D1 and c-Myc mRNA stability in response to rapamycin in an Akt-dependent manner via p38 MAPK signaling.
Oncogene. 2006 May 15 |
| | Smolewski P.
Recent developments in targeting the mammalian target of rapamycin (mTOR) kinase pathway.
Anticancer Drugs. 2006 Jun;17(5):487-94 |
| | Webster AC, Lee VW, Chapman JR, Craig JC.
Target of rapamycin inhibitors (sirolimus and everolimus) for primary immunosuppression of kidney transplant recipients: a systematic review and meta-analysis of randomized trials.
Transplantation. 2006 May 15;81(9):1234-48 |
| | Mercalli A, Sordi V, Ponzoni M, Maffi P, De Taddeo F, Gatti G, Servida P, Bernardi M, Bellio L, Bertuzzi F, Secchi A, Bonifacio E, Piemonti L.
Rapamycin induces a caspase-independent cell death in human monocytes.
Am J Transplant. 2006 Jun;6(6):1331-41 |
| | Kwon YS, Kim JC.
Inhibition of corneal neovascularization by (Sirolimus) rapamycin .
Exp Mol Med. 2006 Apr 30;38(2):173-9 |
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