Anti-Inflammatory Immunosuppressor CAS 104987-11-3 Tacrolimus

1.  Quick Detail:
 
Tacrolimus
Synonyms: (2-propenyl)-,(3s-(3r*(e(1s*,3s*,4s*)),4s*,5r*,8s*,9e,12r*,14r*,15s*,16r*,18s*;,19s*,26ar*))-;16-dimethoxy-4,10,12,18-tetramethyl-8-3-(2-(4-hydroxy-3-methoxycyclohexyl)-1;19-epoxy-3h-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4h,23h)-tetrone,5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-(2-(4-hydroxy-3-methoxycyclohexyl)-14,16-dim;6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-5;fr900506;prograf;tsukubaenolide
CAS: 104987-11-3
MF: C44H69NO12
MW: 804.02
Product Categories:Pharmaceuticals;Chiral Reagents;Fujimycin, Prograf;antibiotic
Chemical Properties: White Crystalline Solid
Assay:99%
Usage: An immunosuppressant that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK-506 binding protein, thereby reversing its effects on sarcoplasmic reticulum Ca+2 release.
Packing:2g/foil bag

2.  Description:

(RAPA) is a new type of large ring lactone class immunosuppressants.Rapamycin factor receptor blocking signal transduction through different cells, block the T cell and other cell from G1 phase to S phase process, thereby immunosuppressive effect into full play.From the point of clinical application, rapamycin has good anti-rejection effect, and with cyclosporine A (CsA) and FK506 immune inhibitors have good synergy, is A kind of good curative effect, low toxicity, no new immunosuppressant nephrotoxicity.In March 2010, the United States, according to a study at the university of Texas rapamycin can be used in the treatment of alzheimer's disease, the drug composition are also present in the Easter island secretion of the bacteria in the soil.
Introduction to the
Rapamycin (Rapamycin, RAPA, RPM), also known as Sirolimus, belongs to the large ring lactone class antibiotic, and F


Rapamycin plus small dose of hormones can be used in the treatment of FSGS
The structure of the K506 similar.
Rapamycin at first been studied as a low toxicity antifungal drug, was discovered in 1977 immunosuppressive effects of rapamycin, beginning in 1989 the RAPA as a rejection of the new drug for the treatment of organ transplantation for trial, at present (2010) I and phase II clinical trial of RAPA has finished, phase III clinical trials are ongoing.
structure
The formulas for rapamycin C51H79NO13, molecular weight of 914.172 g/mol, as white solid crystal, melting point is 183-185 ºC, fatty, soluble in methanol, ethanol, acetone, chloroform and other organic solvents, very slightly soluble in water, hardly soluble in ether.From the results of animal experiment and clinical application of rapamycin is a kind of good curative effect, low toxicity, no new immunosuppressant nephrotoxicity.
Mechanism of action
Rapamycin through different cell factor receptor blocking signaling, T cells and other cells by G1 phase to S phase, the process of rapamycin can T lymphocytes and B lymphocytes of calcium dependency and dependency of calcium signaling pathways.Rapamycin and FK506, combined with the same immune affinity (immunophilin) protein FKBP12 and RAPA - FKBP12 compound formation, the compound can't combine with calmodulin, and rapamycin early also not inhibit T cell activation or directly reduce the synthesis of cytokines.This kind of complex target protein were first identified in yeast, called TOR1 and TOR2.
Recent study found that rapamycin (rapamycin) is a kind of effective autophagy inducers, by inducing autophagy and reduce inflammation, may be one of the play to the mechanism of immunosuppression.
Synthetic route
Rapamycin by seven units of acetate and seven units of propionic acid salt, polyketone synthesis by the O - methyl from methionine.Actually when nitrogen source shikimic acid after reduction of derivatives, from shikimic acid formed in the process of cyclohexane derivatives to retain the integrity of hexamethylene alkyl.Form piperidine carboxylic acid lysine deamination form first, then by piperidine carboxylic acids and polyketone acetyl and amide keys connection, form the initial structure of rapamycin.
The study found that
Study found that rapamycin inhibits the activity of the 70 - KDaS6 kinase (p70S6K), of the enzyme and cell cycle
Is that Easter island secretion of the bacteria in the soil
Many of the key process has a close relationship between different cells.But in cell free system (cell - freesystem), RAPA - but could not inhibit the activity of p70S6K PKBP complex, i.e. RAPA - PKBP complexes with no direct interaction between p70S6K, therefore, speculated that rapamycin may apply to p70S6K before process, inhibit other kinases or activate the phosphatase, the result is that rapamycin inhibition of at least two substrates: (1) promote the synthesis of protein S6 ribosomal proteins, (2) induction of proliferating cell nucleus antigen (PCNA) gene transcription induction cAMP response element regulation factor (CREM).Rapamycin for DNA polymerase delta factor is a necessary process, at the same time in the process of cells to enter S phase also is needed.
 
3.  Specification:
    

Tacrolimus	CAS 104987-11-3	Brand: Hyper
	MW: 804.02	MSDS: Avaiable
	MF : C44H69NO12
	Category:Anti-inflammatory drug	Min order: 10grams
	Quality standard : Enterprise standard	Place of Origin:China
Introduction	Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. Tacrolimus is used to prevent rejection of organ transplants. Tacrolimus is 10 to 100 times superior to cyclosporin in improving graft survival and preventing acute rejection after transplantation, but decreasing the toxin side effects.
Character	A white or off-white crystalline powder
Applications	Pharmaceutical raw materials

4.  Applications:
 
As an ointment, tacrolimus is used in the treatment of eczema, in particular atopic dermatitis. It suppresses inflammation in a similar way to steroids, and is equally as effective as a mid-potency steroid. An important advantage of tacrolimus is that, unlike steroids, it does not cause skin thinning (atrophy), or other steroid related side-effects.
It is applied on the active lesions until they heal off, but may also be used continuously in low doses (twice a week), and applied to the thinner skin over the face and eyelids[citation needed]. Clinical trials of up to one year have been conducted. Recently it has also been used to treat segmental vitiligo in children, especially in areas on the face
 
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