Rapamycin powder (sirolimus powder) is a new type of macrolide immunosuppressant. It is a white powder with a melting point of 183-185°C. It is lipophilic and easily soluble in methanol, ethanol, acetone, chloroform, and other organic Solvent, slightly soluble in water, and almost insoluble in ether. It was developed as early as the 1970s and was originally used as a low-toxicity antifungal drug. It was discovered in 1977 that it has an immunosuppressive effect. Since 1989, RAPA has been tested as a new drug for the treatment of organ transplant rejection. From the results of animal experiments and clinical applications, it is a new type of immunosuppressant with good curative effect, low toxicity, and no nephrotoxicity.
It is a macrolide antibiotic, similar in structure to FK506, but its immunosuppressive mechanism is completely different. FK506 inhibits the proliferation of T lymphocytes from G0 to G1, while Rapamycin blocks signal transduction through different cytokine receptors, blocking the progression of T lymphocytes and other cells from G1 to S. Compared with FK506, Rapamycin can block calcium-dependent and independent signal transduction pathways of calcium-T lymphocytes and B lymphocytes.
It is a macrolide antibiotic derived from actinomycetes, and its structure is similar to FK506. But there are different mechanisms of immunosuppression. Rapamycin blocks signal transduction through different cytokine receptors, such as inhibiting cell proliferation induced by IL-2 and IL-4, IL-1 induced IFN-γ production, and IL-2 and IL-2R induction The expression of the membrane antigen blocks the information transduction pathway after the binding of IL-2 and IL-2r, thereby blocking the process of T lymphocytes and other cells from the G1 phase to the S phase. Compared with FK506, RAPA can block the calcium-dependent and calcium-independent signal transduction pathways of t-lymphocytes and b-lymphocytes.
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| Real shot pictures of Sirolimus powder | Sirolimus structure diagram |
Product Application
1. Rapamycin powder is a new and effective immunosuppressant with anticancer activity.
2. It is a member of the macrolide immunosuppressant family.
3. It is the substrate of cytochrome P450 III A4(CYP3A4) and P- glycoprotein.
4. It is suitable for patients receiving kidney transplantation to prevent organ rejection.
Product Specification
Item | Specification | 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, and 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% |
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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure or prevent any disease.
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