Ascomycin (FK520)

Synonyms: FR 900520, Immunomycin

Ascomycin (FK520, FR 900520, Immunomycin), an FK-506 analog, is a neutral macrolide immunosuppressant, which prevents rejection after an organ transplant. Phase 3.

Ascomycin (FK520) Chemical Structure

Ascomycin (FK520) Chemical Structure

CAS: 104987-12-4

Selleck's Ascomycin (FK520) has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.71%
99.71

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Choose Selective Anti-infection Inhibitors

Biological Activity

Description Ascomycin (FK520, FR 900520, Immunomycin), an FK-506 analog, is a neutral macrolide immunosuppressant, which prevents rejection after an organ transplant. Phase 3.
Targets
calcineurin phosphatase [2]
49 nM
In vitro
In vitro Ascomycin, isolated from Streptomyces, suppresses immune response in vitro with IC50 of 0.55 nM for mouse mixed lymphocyte. [1] 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. [2] Ascomycin shows antimalarial effects via inhibition of the chaperone activity of this bifunctional protein. [3]
In Vivo
In vivo Ascomycin (3.2 mg/kg, i.m.) clearly prolongs skin allograft survival in rats. [1] Ascomycin, at 50 or 100 μM, produces anticonvulsant effect against picrotoxin-induced seizures when infused into the rat hippocampus. [4]
Animal Research Animal Models Recipient WKA rats transplanted with F344 skin allografts.
Dosages ~32 mg/kg 5 days a week.
Administration i.m.

Chemical Information & Solubility

Molecular Weight 792.01 Formula

C43H69NO12

CAS No. 104987-12-4 SDF Download Ascomycin (FK520) SDF
Smiles CCC1C=C(CC(CC(C2C(CC(C(O2)(C(=O)C(=O)N3CCCCC3C(=O)OC(C(C(CC1=O)O)C)C(=CC4CCC(C(C4)OC)O)C)O)C)OC)OC)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (126.26 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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