CAS number：53123-88-9
molecular formula：C51H79NO13
molecular weight：914.19
EINECS number：610-965-5

English synonyms

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

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Introduction

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. According to the effect of clinical application, it is a new type of immunosuppressant with good efficacy, 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). ). They are quite interested that the main component of rapamycin is also present in bacterial products in the isolated soil of Easter Island. The latest experiments show 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 Procofo (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, blocking 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.

Chemical properties

Use

●  In recent years, studies have found that the target of rapamycin (mTOR) is an intracellular kinase, and the abnormality of its conduction pathway can induce a variety of diseases. As a targeted inhibitor of mTOR, rapamycin can treat tumors closely related to this pathway, including renal cancer, lymphoma, lung cancer, liver cancer, breast cancer, neuroendocrine cancer and gastric cancer. Especially in the treatment of two rare diseases, LAM (lymphangiomyomatosis) and TSC (tuberous sclerosis), the effect is more obvious, and LAM and TSC can also be regarded as tumor diseases to some extent.

●  as an immunosuppressant

●  A triene macrolide antibiotic isolated from Streptomyces hygroscopicus. Name derived from the native word for Easter Island, Rapaui. Used as an immunosuppressant; antirestenotic. Sirolimus (INN/USAN ), also known as rapamycin, is an immunosuppressant drug used to prevent rejection in organ transplantation; it is especially useful in kidney transplants.

●  A member of the macrolide immunosuppressant family. FRAP inhibitors. Binds and inhibits the target of rapamycin (mTOR). A potent immunosuppressant with anticancer activity.