Pharmaceutical Tacrolimus and Fk506 CAS 104987-11-3 for Immunosuppressive

Details:

1. Quick Detail:

Tacrolimus
Synonym: FK-506, FK506, Fujimycin; FR-900506; [(E)-2-[(1R, 3R, 4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14, 16-; Tacrolimus (FK506);
Purity: 99%
CAS No.: 104987-11-3
Grade: Pharmaceutical Grade
Place of Origin: Wuhan, China
Delivery time: Usually 4-6 working days by air
Storage: Store in a cool, dry place. Do not store in direct sunlight. Store in a tightly closed container.


2. Product description:

MF: C44H69NO12
MW: 804.02
Assay ≥ 99.0%
Density: 1.19 g/cm3
Melting Point: 113-115° C
Boiling Point: 871.7 ° C at 760 mmHg
Vapour: 1.73E-35mmHg at 25° C
Refractive Index: 1.549
Flash Point: 481 ° C
Water: DMSO: >3 mg/mL
Solubilities: DMSO: >3 mg/mL
Appearance: White or off-white crystalline powder


3. Application
L Immunosuppression following transplantation
It has similar immunosuppressive properties to ciclosporin, but is much more potent. Immunosuppression with tacrolimus was associated with a significantly lower rate of acute rejection compared with ciclosporin-based immunosuppression (30.7% vs 46.4%) in one study. Clinical outcome is better with tacrolimus than with ciclosporin during the first year of liver transplantation. Long term outcome has not been improved to the same extent. Tacrolimus is normally prescribed as part of a post-transplant cocktail including steroids, mycophenolate and IL-2 receptor inhibitors. Dosages are titrated to target blood levels. Typical starting doses for once daily tacrolimus are 0.15-0.20 mg/kg body weight.
L Interactions
Also like cyclosporin it has a wide range of interactions, including that with grapefruit which increases plasma-tacrolimus concentration. Several of the newer class of antifungals, especially of the azole class (fluconazole, posaconazole) also increase drug levels by competing for degradative enzymes.
L Ulcerative colitis
In recent years, tacrolimus has been used to suppress the inflammation associated with ulcerative colitis, a form of inflammatory bowel disease. Although almost exclusively used in trial cases only, tacrolimus has shown to be significantly effective in the suppression of outbreaks of UC.
L Dermatological use
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