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Moisture Sensitive Rapamycin Powder High Purity Cas 53123-88-9 Macrolides Immunosuppressant

Basic Information
Place of Origin: China
Brand Name: rapamycin online
Certification: ISO
Model Number: rapamycin
Minimum Order Quantity: 10 grams
Price: Inquiry
Packaging Details: 1kg/bag;25kg/Durm
Delivery Time: 1-3work days
Payment Terms: T/T, Western Union, MoneyGram
Supply Ability: 5000kg per Month
Detail Information
Name: Rapamycin For Sale CAS: 53123-88-9
EINECS: 610-965-5 Keyword: Rapamycin
Merck : 14,8114 Sensitivity: Moisture Sensitive/Light Sensitive/Hygroscopic
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Product Description

In stock high purity rapamycin powder Cas 53123-88-9 sale online

 

Rapamycin Description
Rapamycin (RAPA) is a new macrolides immunosuppressant, white solid crystal, melting point of 183-185℃, lipophile, dissolved in methanol, ethanol, acetone, chloroform and other organic solvents, very slightly soluble in water, almost insoluble in ether.
Was developed in the early 1970 s, initially was as low toxicity antifungal drugs, immunosuppressive effects of discovery in 1977, started in 1989 the RAPA as a rejection of the new drug for the treatment of organ transplantation in trial, look from animal experiment and clinical application effect, is a kind of good curative effect, low toxicity, no new immunosuppressant nephrotoxicity.
While it is often used as a drug to maintain the immune capacity of transplanted organs (especially kidney transplants) to slow the immune rejection response after organ transplantation, scientists have recently found another use for it: to treat alzheimer's disease.
Interestingly, the main component of rapamycin was also found in the bacterial product of the isolated soil on Easter island, and recent experiments showed that it restored the ability to remember defects in mice.
Rapamycin is a macrolide antichemicalbook, similar in structure to prozac (FK506), but with very different immunosuppressive mechanisms.
FK506 inhibits the proliferation of T lymphocytes from G0 to G1, while RAPA blocks the signaling process of T lymphocytes and other cells from G1 to S through different cytokine receptors. Compared with FK506, RAPA blocks calcium-dependent and non-calcium-dependent signaling pathways of T lymphocytes and B lymphocytes.
Medical researchers at the university of Chicago used commercially available oral rapamycin tablets combined with grapefruit juice to treat melanoma, a malignant cancer common in Europe and the United States, to significantly improve the anti-cancer effects of other chemotherapy drugs and thus prolong survival.
Studies have shown that rapamycin is easily decomposed by enzymes after entering the digestive tract, while grapefruit juice contains a large amount of furanocoumarins, which can inhibit the destruction of rapamycin by enzymes in the digestive tract, thus improving the bioavailability of rapamycin.
It is said that the earliest Dutch doctors have found: grapefruit juice has the effect of improving the oral absorption of mountain Ming, now European and American doctors will be applied to rapamycin preparations.

Rapamycin Function

Rapamycin is a member of the macrolide immunosuppressant family and a FRAP inhibitor. Rapamycin exhibits binding and inhibitory actions to the FK506 binding protein (FKBP5) proline rotamase via simultaneous binding by FKBP12 and FRAP. FRAP (RAFT1) proteins exhibit homology to PI 4- and PI 3-kinases, which have PI 4-kinase and autophosphorylating activities.The rapamycin/FKBP complex does not inhibit the FRAP PI 4-kinase activity, but does inhibit FRAP autophosphorylation. Rapamycin is unique in its ability to inhibit lymphokine induced cell proliferation at the G1 and S phase as well as an irreversible cellular arrest at the G1 phase in S. cerevisiae cells. It also exhibits selective signal blocking leading to the activation of p70/85 S6 kinase, which is potentially due to the inhibition of FRAP autophosphorylation or protein kinase activity. Angiogenesis inhibition is also exhibited,possibly through the inhibition of the Akt pathway. Rapamycin is an inhibitor of mTOR.

Rapamycin Application

The combination of Rapamune with cyclosporine and corticosteroids is recommended.
Rapamune is given orally once a day.
After transplantation, Rapamune should be started as early as possible.
For new transplant recipients, the first dose of Rapamune should be three times its maintenance dose.
The recommended load for renal transplant patients is 6mg and the maintenance dose is 2mg/ day.
Although the 15mg load and 5mg/ d maintenance dose used in clinical trials were safe and effective, the efficacy of a dose above 2mg in kidney transplant patients is unclear.
The overall safety of patients taking 2 mg of Rapamune daily was better than that of patients taking 5 mg of Rapamune daily.
To minimize Rapamune absorption differences, the drug should be taken consistently with or without food.
Grapefruit juice slows down the metabolism of Rapamune, which is regulated by CYP3A4, so it should not be used for serving or thinning Rapamune.
It is recommended to take siromos 4 hours after taking the cyclosporine oral solution (improved) (e.g., Neoral solution, SangCya oral solution) and/or cyclosporine capsules (improved).
Rapamycin Specification
PRODUCT NAME Rapamycin
Batch number ACT20191228 Quantity 7.6kg
Storage Sealed to keep away from moisture
Items of analysis Specification Results
Appearance White powder Conforms
Identification Meet the requirements Conforms
PH 2.4~3.0 2.60
Loss on drying ≤0.5% 0.04%
Sulphated ash ≤0.1% 0.01%
Heavy metals ≤20 ppm <20 ppm
Related substances ≤0.25% Conforms
Residue on ignition ≤0.1% 0.01%
Residue solvent - Ethanol ≤0.5% <0.06%
Assay 99.0%~101.0% 99.6%

 

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