product name Ascomycin (FK520)
Description: Ascomycin (also known as FK520, FR 900520, Immunomycin), isolated from Streptomyces, is an FK-506 analog and a neutral macrolide immunosuppressant, which prevents rejection after an organ transplant. Ascomycin suppresses immune response in vitro with IC50 of 0.55 nM for mouse mixed lymphocyte. Ascomycin inhibits calcineurin phosphatase with IC50 of 49 nM through formation of an FKBP12-FK520-calcineurin ternary complex.
References: J Antibiot (Tokyo). 1988 Nov;41(11):1592-601; J Pharmacol Exp Ther. 2002 Sep;302(3):1278-85.
792.01
Formula
C43H69NO12
CAS No.
104987-12-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (126.3 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (126.3 mM)
Solubility (In vivo)
Synonyms
FR 900520, Immunomycin
other peoduct :
| In Vitro |
In vitro activity: Ascomycin, isolated from Streptomyces, suppresses immune response in vitro with IC50 of 0.55 nM for mouse mixed lymphocyte. Ascomycin inhibits calcineurin phosphatase with IC50 of 49 nM through formation of an FKBP12-FK520-calcineurin ternary complex. FK520 also accelerate the rate of nerve regeneration, and promotes neurite outgrowth. Ascomycin shows antimalarial effects via inhibition of the chaperone activity of this bifunctional protein. Kinase Assay: Cell Assay: Ascomycin (FK 520, FR900520) suppressed lymphocyte reaction in a dose dependent fashion. Ascomycin was non-toxic at concentrations less than 3,200 nM, at which the percent inhibition was 18.9%. Ascomycin showed antifungal activity against Aspergillus fumigatus IFO 5840. Ascomycin had no inhibitory effect on bacteria or yeast at 100 μg/ml. |
|---|---|
| In Vivo | Ascomycin (3.2 mg/kg, i.m.) clearly prolongs skin allograft survival in rats. Ascomycin, at 50 or 100 μM, produces anticonvulsant effect against picrotoxin-induced seizures when infused into the rat hippocampus. |
| Animal model | Recipient WKA rats transplanted with F344 skin allografts. |
| Formulation & Dosage | Dissolved in Olive oil; 32 mg/kg 5 days a week; i.m. injection |
| References | J Antibiot (Tokyo). 1988 Nov;41(11):1592-601; J Pharmacol Exp Ther. 2002 Sep;302(3):1278-85; Pharmacol Biochem Behav. 2006 Jul;84(3):511-6. |
