104987-12-4 Ascomycin AKSci L987
 
 
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  L987    
Ascomycin
, 95% (HPLC)
 
Immunomycin, FR-900520, FK-520




IDENTITY
CAS Number:104987-12-4
MDL Number:MFCD06198665
MF:C43H69NO12
MW:792.0075
SPECIFICATIONS & PROPERTIES
Purity:95% (HPLC)
Spectra:FT-IR, LCMS, HPLC
Physical Form:White crystalline powder
Melting Point:155-157°C
Long-Term Storage:Store long-term at -20°C
UN #:Not hazmat

BIOLOGICAL INFO
Application(s):An immunosuppressive antibiotic FK506 analog

REVIEW

 Ascomycin is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. IC50 Value: 0.55 nM. Target: in vitro: When we used either CD4+CD8+ thymocytes or peripheral T cells activated by phorbol ester and ionomycin, the cell surface induction of CD5 was also partially blocked by CsA, FK-520 and rapamycin. Ascomycinalso had a 3-fold lower immunosuppressive potency in a popliteal lymph node hyperplasia assay, resulting in an equivalent therapeutic index consistent with a common mechanistic dependence on calcineurin inhibition. in vivo: In 14-day studies, nephrotoxicity was not induced by continuous i.p. infusion of ascomycin at 10 mg/kg/day or daily oral administration (up to 50 mg/kg/day) in rats on a normal diet, nor by continuous i.v. infusion (up to 6 mg/kg/day) in rats on a low salt diet to enhance susceptibility.

REFERENCES
[1]Mollison KW, Fey TA, Krause RA, Nephrotoxicity studies of the immunosuppressants tacrolimus (FK506) and ascomycin in rat models. Toxicology. 1998 Feb 6;125(2-3):169-81.
[2] Teutsch M, Higer M, Wang D, Induction of CD5 on B and T cells is suppressed by cyclosporin A, FK-520 and rapamycin. Int Immunol. 1995 Mar;7(3):381-92.
[3] Hatanaka H, Kino T, Miyata S, FR-900520 and FR-900523, novel immunosuppressants isolated from a Streptomyces. II. Fermentation, isolation and physico-chemical and biological characteristics. J Antibiot (Tokyo). 1988 Nov;41(11):1592-601.

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


Current as of January 18, 2019


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CATEGORIES

 APIs and Bioactives > Immunomodulators


PubChem