Rapamycin Powder CAS 53123-88-9

Rapamycin powder(RAPA) is a new macrolide immunosuppressant. It is a white strong crystal with a melting point of 183-185 ° C. It is lipophilic and soluble in methanol, ethanol, acetone, chloroform and also other natural solvents. It is extremely slightly soluble in water and also virtually insoluble in ether. It was established as early as the 1970s. It was originally used as a low-toxic antifungal drug. In 1977, it was found that it had immunosuppressive results. In 1989, RAPA was utilized as a new medicine for the therapy of body organ transplant rejection. From the results of animal experiments and professional applications, it is a new kind of immunosuppressant with good curative effect, reduced poisoning, as well as no nephrotoxicity. Now it is typically utilized as a medication to preserve the immunity of hair transplanted body organs (specifically kidney transplantation) to slow down the immune being rejected after organ transplantation. However, researchers have recently uncovered an additional use for it: it can be utilized to treat Alzheimer’s illness (senile dementia). What interested them was that the major part of rapamycin powder was additionally present in the microbial item of the isolated soil of Easter Island. The latest experiments revealed that the substance can bring back memory shortages when provided to speculative computer mice.

Rapamycin powder is a macrolide antibiotic, which has a similar framework to Prograf (FK506), but has a very various immunosuppressive system. FK506 hinders the spreading of T lymphocytes from G0 stage to G1 phase, while RAPA blocks signal transduction through different cytokine receptors, blocking the progress of T lymphocytes as well as various other cells from G1 phase to S phase. Compared to FK506, RAPA can obstruct the calcium-dependent and calcium-independent signaling pathways of T lymphocytes and also B lymphocytes.

Scientists at the University of Chicago Medicine utilized commercially offered rapamycin dental tablets plus grapefruit juice to deal with cancer malignancy (a common deadly lump condition in Europe and the United States), which can substantially improve the anticancer effect of other radiation treatment drugs, thereby extending the survival time of patients. Researches have actually shown that rapamycin is easily decayed by enzymes after getting in the digestion tract, and grapefruit juice contains a large quantity of furanocoumarins, which can prevent the devastation of rapamycin by digestive system enzymes, so it can improve the bioavailability of rapamycin. It is claimed that the earliest Dutch medical professionals have actually uncovered that grapefruit juice can boost the oral absorption impact of Sandimin, as well as currently doctors in Europe and also the USA apply it to rapamycin preparations.