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Ascomycin (FK520) Anti-infection chemical

Cat.No.S7411

Ascomycin (FK520, FR 900520, Immunomycin), an FK-506 analog, is a neutral macrolide immunosuppressant that prevents rejection after an organ transplant. Phase 3.
Ascomycin (FK520) Anti-infection chemical Chemical Structure

Chemical Structure

Molecular Weight: 792.01

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Quality Control

Batch: Purity: 99.71%
99.71

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (126.26 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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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Chemical Information, Storage & Stability

Molecular Weight 792.01 Formula

C43H69NO12

Storage (From the date of receipt)
CAS No. 104987-12-4 Download SDF Storage of Stock Solutions

Synonyms FR 900520, Immunomycin 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

Mechanism of Action

Targets/IC50/Ki
calcineurin phosphatase
49 nM
In vitro
Ascomycin (FK520), isolated from Streptomyces, suppresses immune response in vitro with IC50 of 0.55 nM for mouse mixed lymphocyte. It inhibits calcineurin phosphatase with IC50 of 49 nM through formation of an FKBP12-FK520-calcineurin ternary complex. This compound also accelerates the rate of nerve regeneration, and promotes neurite outgrowth. It shows antimalarial effects via inhibition of the chaperone activity of this bifunctional protein.
In vivo
Ascomycin (FK520) (3.2 mg/kg, i.m.) clearly prolongs skin allograft survival in rats. When infused into the rat hippocampus at 50 or 100 μM, this compound produces anticonvulsant effect against picrotoxin-induced seizures.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16872668/

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