| Customization: | Available |
|---|---|
| Powder: | Yes |
| Customized: | Customized |
|
Still deciding? Get samples of $ !
Request Sample
|
Suppliers with verified business licenses
Rapamycin (RAPA) is a new type of macrolide immunosuppressant. It is a white solid crystal with a melting point of 183-185ºC. It is lipophilic and soluble in organic solvents such as ethanol. It is slightly soluble in water and almost insoluble in ether. RAPA was developed as early as the 1970s and was initially used as a low-toxicity antifungal drug. In 1977, it was discovered to have immunosuppressive effects. In 1989, RAPA began to be tested as a new drug for treating organ transplant rejection. Judging from the effects of animal experiments and clinical applications, it is a new type of immunosuppressant with good efficacy, low toxicity and no nephrotoxicity. Nowadays, it is often used as a drug to maintain the immune capacity of transplanted organs (especially in kidney transplants) to slow down the immune rejection reaction after organ transplant surgery. However, scientists have recently discovered another use of it: it can be used to treat Alzheimer's disease. What interests them quite a lot is that the main component of rapamycin also exists in the bacterial products isolated in the soil of Resurrection Island. The latest experiments show that when this substance is applied to the affected experimental mice, it can restore the ability of memory deficiency.
Discover history
Rapamycin (also known as "sirolimus") is a secondary metabolite secreted by Streptomyces soil, which was first discovered by scientists in the soil of Easter Island, Chile in 1975. Its chemical structure belongs to "triene macrolide" compounds. Due to factors such as the low fermentation yield of rapamycin and the complex extraction process, this product was not developed and launched by the American Household Chemicals Company until 1999, and was subsequently launched in more than ten countries in Europe and America.
At that time, the U.S. Food and Drug Administration (FDA) approved the indication of rapamycin not as an antibiotic but as an "immunosuppressant". This is because rapamycin has shown a powerful immunosuppressive effect in clinical trials and can replace cyclosporine, which has a clinical history of more than 30 years. Moreover, compared with cyclosporine, rapamycin oral liquid has a smaller dosage (only 2 to 3mg each time), a stronger anti-rejection effect, and fewer side effects. Therefore, since its launch, rapamycin has quickly become a commonly used oral immunosuppressant for organ transplant recipients around the world.
Side effects
Rapamycin (RAPA) has similar side effects to FK506. In a large number of clinical trials, it has been found that its side effects are dose-dependent and reversible. No obvious nephrotoxicity has been found in therapeutic doses of RAPA, and there is no gingival hyperplasia. The main toxic and side effects include: headache, nausea, dizziness, nosebleeds and joint pain. Abnormal laboratory tests include: thrombocytopenia, leukopenia, decreased hemoglobin, hypertriglyceridemia, hypercholesterolemia, hyperglycemia, elevated liver enzymes (SGOT, SGPT), elevated lactate dehydrogenase, hypokalemia, hypomagnesemia, etc. Recently, it has been reported that taking RAPA can cause eyelid edema, and the reason for the low plasma phosphate level is believed to be that RAPa-based immunosuppressive therapy prolongs the excretion of phosphate from the transplanted kidney. Like other immunosuppressants, RAPA has an increased chance of infection. It has been reported that there is a particular tendency to increase pneumonia, but the occurrence of other opportunistic infections is not significantly different from that of CsA.
Purpose
Member of the macrolide immunosuppressant family. FRAP inhibitor. Bind and inhibit the target molecule of rapamycin (mTOR). A powerful immunosuppressant with anti-cancer activity.
){kind=link}