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Synonyms:AY 22989;23,27-EPOXY-3H-PYRIDO(2,1-C)(1,4)OXAAZACYCLOHENTRIACONTINE;NSC-226080;RAPA;RAPAMUNE;RAPAMYCIN;RAPAMYCIN, STREPTOMYCES HYGROSCOPICUS;RPM
alpha D25 -58.2° (methanol)
Flash point:87 °C
storage temp. -20°C
solubility ethanol: soluble2MM
color colorless to yellow
Water Solubility Soluble in DMSO at 50mg/ml or methanol at 25mg/mlSoluble in alcohol, dimethyl sulfoxide and dimethylformamide. Insoluble in water.
Sensitive Moisture Sensitive/Light Sensitive/Hygroscopic
Sirolimus Rapamycin ,A triene macrolide antibiotic isolated from streptomyces hygroscopicus.Name derived from the native word for easter island, rapa'nui.Used as an immunosuppressant;Antirestenotic.Rapamycin is a triene macrolide discovered in 1995 as a metabolite of streptomyces hygroscopicus found in a soil obtained on rapi nui (easter island).Rapamycin displayed potent and selective antifungal activity, notably against candida albicans. Interest in the metabolite waned until the structural relationship to the potent immunosuppressant fujimycin (antibiotic fk506) was recognised in the mid-1980s.
Sirolimus Rapamycin ,This recognition led to the re-discovery of rapamycin as a highly selective antitumour and immunosuppressant. Rapamycin inhibits the activity of the protein, mtor (mammalian target of rapamycin) which functions in a signalling pathway to promote tumour growth.Rapamycin binds to a receptor protein (fkbp12).The rapamycin/fkb12 complex then binds to mtor and prevents interaction of mtor with target proteins in this signalling pathway.
off-white to yellow crystalline powder
The IR spectrum of Potassium Bromide preparation of the sample exhibits maxima at the same wavelengths as that of a similar preparation of in-house reference standard
The UV spectrum of 95% Ethanol preparation of the sample exhibits maxima at 267nm,277nm, 288nm that of similar preparation of in-house reference standard.
The retention times of the peaks for the Trans- and Cis-stereoisomers in the chromatogram of Assay preparation corresponds to that in the chromatogram of the standard preparation, as obtained in the Assay
Loss on drying
Cis-stereoisomer of Sirolimus
Sirolimus is indicated for the prevention of organ transplant rejection and for the treatment oflymphangioleiomyomatosis
Rapamycin initially was taken as low toxicity antifungal drugs, and was found immunosuppressive in 1977. From 1989, RAPA was as a new drug for the treatment of organ transplantation rejection in trial, and from animal experiments and clinical application effects, it is of good curative effects, low toxicity and no new immunosuppressant nephrotoxicity.
Now rapamycin is frequently as maintaining immunity drug for transplant organs (especially kidney transplant), to slow down the immune rejection of the organ in transplant surgery, however, scientists recently discovered another purpose: it can be used in the treatment of alzheimer's disease (senile dementia).
Medical researchers from University of Chicago combined commercially available rapamycin oral tablets with grapefruit juice in the treatment of melanoma (a kind of malignant tumor disease common in European and American people), which could greatly improve the anticancer effect of other chemotherapy drugs, thereby prolong the survival time of patients.