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Rapamycin Pharmaceutical Intermediates
Rapamycin Pharmaceutical Intermediates

Rapamycin Pharmaceutical Intermediates

Contact : Mr.Thyen-------------------------------- Email us at zhangyinglong@ycphar.com Whatsapp : +86 180 3817 6818

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Rapamycin


Contact : Mr.Thyen

Email us at zhangyinglong@ycphar.com

Whatsapp : +86 180 3817 6818



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CAS:53123-88-9

MF:C51H79NO13

MW:914.18

EINECS:262-640-9

Synonyms:AY 22989;23,27-EPOXY-3H-PYRIDO(2,1-C)(1,4)OXAAZACYCLOHENTRIACONTINE;NSC-226080;RAPA;RAPAMUNE;RAPAMYCIN;RAPAMYCIN, STREPTOMYCES HYGROSCOPICUS;RPM

 

Properties

Melting point:183-185°C

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


Abstract

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.

 

Specification

Item

Specifications

Results

Description

off-white to yellow crystalline powder

Complies


     Identification

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

Complies

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.

Complies

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

Complies

Loss on drying

≤0.5%

0.16%

Heavy metal

≤0.002%

Complies

Total impurity

≤2.0%

0.76%

Single impurity

≤1.0%

0.67%

Cis-stereoisomer of Sirolimus

≤5.0%

2.4%

Assay

≥98.0%

99.2%


Clinical Function

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.

 

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