Rapamycin CAS 53123-88-9

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Rapamycin (RAPA) is a new type of macrolide immunosuppressant. It is a white solid crystal with a melting point of 183-185 °C. It is lipophilic and can be dissolved in organic solvents such as methanol, ethanol, acetone, and chloroform. Soluble in water, almost insoluble in ether. It was developed as early as the 1970s. It was initially used as a low-toxic antifungal drug. In 1977, it was found to have immunosuppressive effects. In 1989, RAPA was used as a new drug for the treatment of organ transplant rejection. In terms of clinical application, it is a new type of immunosuppressant with good curative effect, low toxicity and no nephrotoxicity. It is now often used as a drug to maintain the immunity of transplanted organs (especially kidney transplants) to slow down the immune rejection after organ transplants. However, scientists have recently discovered another use for it: it can be used to treat Alzheimer's disease (senile dementia). ). What interested them was that the main component of rapamycin was also present in bacterial products in the isolated soil of Easter Island. The latest experiments showed that the application of this substance to the experimental mice can restore the ability of memory defects. Rapamycin is a macrolide antibiotic that is structurally similar to Procofol (FK506), but has a very different immunosuppressive mechanism. FK506 inhibits the proliferation of T lymphocytes from G0 phase to G1 phase, while RAPA blocks signaling through different cytokine receptors and blocks the progression of T lymphocytes and other cells from G1 phase to S phase, compared with FK506 , RAPA can block calcium-dependent and calcium-independent signaling pathways of T and B lymphocytes. University of Chicago medical researchers use commercially available oral rapamycin tablets plus grapefruit juice to treat melanoma (a common malignant tumor disease in Europe and the United States), which can greatly improve the anticancer effect of other chemotherapy drugs, thereby prolonging the survival of patients time. Studies have shown that rapamycin is easily decomposed by enzymes after entering the digestive tract, and grapefruit juice contains a large amount of furanocoumarins, which can inhibit the destructive effect of digestive tract enzymes on rapamycin. Can improve the bioavailability of rapamycin. It is said that the earliest Dutch doctors have discovered that grapefruit juice can improve the oral absorption effect of Shanming, and now doctors in European and American countries have applied it to rapamycin preparations.

Sirolimus, also known as rapamycin, is a macrolide produced by the bacteria Streptomyces hygroscopicus. It has immunosuppressant functions in humans and is used to prevent rejection in organ transplantation; it is especially useful in kidney transplants. It prevents activation of T cells and B cells by inhibiting their response to interleukin-2 (IL-2). Sirolimus is also used as a coronary stent coating. Sirolimus works, in part, by eliminating old and abnormal white blood cells. Sirolimus is effective in mice with autoimmunity and in children with a rare condition called autoimmune lymphoproliferative syndrome (ALPS).
A growing body of evidence has demonstrated that although limited, rapamycin or rapalogs are beneficial for treating various diseases including cancer, diabetes, tuberous sclerosis complex, lymphangioleiomyomatosis, neurodegenerative diseases and aging.

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