Rapamycin Powder CAS 53123-88-9
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- Appearance: White powder
- Purity: 99. 0%min
- Stock: In stock
- Sample: Available
- Zhishang Chemical: Rapamycin Powder Supplier & Manufacturer
Rapamycin Powder: The Complete Guide
Rapamycin Powder for Sale
|Chemical Name:||Rapamycin Powder|
|Other Name:||Rapamycin; Sirolimus; DMF; GMP|
|Type:||Pharmaceutical raw materials; Pharmaceutical intermediates; Synthetic material intermediates; Plant extracts|
What is Rapamycin Powder?
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.
Rapamycin Powder Uses
- Member of the macrolide immunosuppressant household. FRAP preventions. Binds and also prevents target of rapamycin (mTOR). A potent immunosuppressant with anticancer task.
- Sirolimus is a sort of Macrolide antibiotic, similar to FK506 in framework, however various in immunosuppressive device. FK506 hinders the expansion of T lymphocytes from G0 phase to G1 phase, while RAPA obstructs signal transduction by utilizing various Cytokine receptor, hence avoiding T lymphocytes and also other cells from multiplying from G1 stage to S phase. Compared to Prograf, Sirolimus can obstruct the calcium reliant as well as calcium independent signal transduction paths of T and also B lymphocytes.
- Research studies in recent years have actually discovered that the target of rapamycin (mTOR) is an intracellular kinase, and the problem of its transduction pathway can cause different illness. As a targeted inhibitor of mTOR, rapamycin can treat lumps carefully pertaining to this pathway, consisting of renal cancer, lymphoma, lung cancer cells, liver cancer, breast cancer, neuroendocrine cancer cells and stomach cancer. Especially in the therapy of 2 unusual illness, LAM (lymphangioleiomyomatosis) as well as TSC (tuberous sclerosis), which can likewise be thought about as neoplastic illness to some extent.
- As an mTOR prevention, sirolimus has a large range of activities as well as has been shown to hinder swelling, spreading, angiogenesis, fibrosis, and high permeability. Sirolimus has lots of usages in the prevention of body organ Transplant denial and recently in the treatment of sophisticated kidney cell cancer. Sirolimus eluting heart stents have actually been shown to restrict the rate of tissue overgrowth as well as prevent coronary artery restenosis. Very early researches have shown that it might be a reliable medication to control extreme Uveitis, as well as might additionally contribute in the therapy of age-related Macular deterioration.
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Pharmacological Action and Mechanism of Sirolimus
Sirolimus and FK506 are structural homologues, although they act on the same receptor, their immune mechanism of action is different. FK506 inhibits the proliferation of T lymphocytes from G0 phase to G1 phase, while sirolimus blocks signal transduction through different cytokine receptors and blocks the progress of T lymphocytes and other cells from GI phase to S phase. Compared with FK506, sirolimus can block the calcium-dependent and calcium-independent signaling pathway P1 of T lymphocytes and B lymphocytes. Current research shows that: FK506 and cyclosporin A produce immunosuppressive effects by inhibiting calcineurin, while sirolimus inhibits the immune function of the body by affecting unique cell signaling pathways.
Sirolimus and FK506 share the same receptor in the body, that is, FK506 immune binding protein (FKBP). After sirolimus binds to FKBP, on the one hand, it inhibits the activation of 70-KSU6 kinase (p7), so that ribosomal 40S subunit S6 protein cannot phosphorylate g7 to affect protein synthesis; on the other hand, it inhibits cyclin D2, D3 and cell cycle-dependent kinase cdk4 , the expression of cdk6 and the activation of Cyclin E-cdk2 complex make the cells stagnate in the middle and late stages of GI, and cannot continue to proliferate. Its direct target may be a protein mammalian ‘ rOR (mTOR) with a homologous sequence to phospholipid phthaloinositide kinase, that is, the combination product of sirolimus and FKBP complex and mTOR can block the immune response triggered by H, -2, U, -15 or CD28/B7 co-stimulatory pathway activation of mTOR, thus exerting a powerful immunosuppressive effect.
Adverse Reactions of Sirolimus
The adverse reactions of this product mainly include the following three aspects:
- European multi-center sirolimus clinical research found that the incidence of hypercholesterolemia in the product group and the control group were 44% and 14%, respectively. The incidence of hypertriglyceridemia in this product and the control group were 51% and 12% respectively. The hyperlipidemia was more obvious when the drug concentration was higher (>30μg/L), and the hyperlipidemia could be significantly improved with the decrease of the drug dose and blood concentration.
- Bone marrow suppression: After taking this product, there may be bone marrow suppression such as decreased platelet and white blood cell counts, decreased hemoglobin levels, etc., but this change is dose-dependent, and can often return to normal after reduction or drug withdrawal. The mechanism is not clear, and it may be related to the inhibition of signal transmission of certain growth factor receptors.
- Liver damage: After using this product, liver function damage may occur, mainly manifested as a significant increase in transaminases. In addition, oral administration of a small dose of this product 1mg/d-2mg/d can cause adverse reactions such as headache, multiple arthralgia, mild gastritis, diarrhea, and acne. Like other immunosuppressants, this product can also cause excessive immunosuppression, leading to infection and tumors. However, compared with CSA and FK506, the biggest advantage of wood products is that they have no nephrotoxicity and neurotoxicity.
- Rapamycin – an overview | ScienceDirect Topics
- Zhu Man, Guo Daihong. A new macrolide immunosuppressant-sirolimus[J]. Chinese Drug Application and Monitoring, 2005 (6): 26-28.
- Yang Can, Liu Baoshan. A new type of high-efficiency, multi-activity and low-toxicity immunosuppressant—new research progress of sirolimus[J]. Strait Pharmacy, 2003, 15(5): 1-4.
Rapamycin Powder Supplier and Manufacturer
As a rapamycin powder supplier and manufacturer with a strict standard product quality system certificate, Zhishang Chemical has long been providing the best rapamycin powder raw materials to customers all over the world.
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