research use only
Cat.No.S3742
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In vitro |
DMSO
: 81 mg/mL
(198.25 mM)
Ethanol : 28 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.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 408.57 | Formula | C24H40O5 |
Storage (From the date of receipt) | |
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| CAS No. | 81-25-4 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CC(CCC(=O)O)C1CCC2C1(C(CC3C2C(CC4C3(CCC(C4)O)C)O)O)C | ||
| In vitro |
Fosfomycin is known to inhibit MurA by covalently binding to a highly conserved cysteine in the active site of the enzyme. Fosfomycin is a PEP mimetic that acts by alkylating the highly conserved Cys115 (Escherichia coli numbering) of MurA. Fosfomycin exerts immunomodulatory effects by altering lymphocyte, monocyte and neutrophil function. It affects the acute inflammatory cytokine response in vitro and in vivo. It suppresses production of tumor necrosis factor alpha (TNF-α), interleukin-1β (IL-1β), and IL-1α and increases production of IL-10. Fosfomycin suppresses IL-2 production from T cells, the production of leukotriene B4 (LTB4) from neutrophils, and the expression of IL-8 mRNA by LTB4 from monocytes. Fosfomycin also exhibits an immunomodulatory effect on B-cell activation. Fosfomycin enhances neutrophil phagocytic killing of invading pathogens, even in patients on chronic hemodialysis and renal transplantation. Fosfomycin resulted in enhanced bactericidal ability of neutrophils compared to other antimicrobials. Fosfomycin has the ability to penetrate into biofilms. fosfomycin is considerably active against both Gram-negative and Gram-positive pathogens.
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| In vivo |
The oral bioavailability of fosfomycin trometamol ranges between 34 and 58%. Absorption occurs in the small intestine, and evidence suggests that coadministration of fosfomycin trometamol with food may reduce absorption of the drug.The mean serum elimination half-life (t1/2) of fosfomycin trometamol is estimated at 5.7 h. Fosfomycin is excreted nonmetabolized in the urine, through glomerular filtration. Depending on age, fasting, and renal function, 11 to 60% of the drug can be found in the urine within 24 h from administration. Specifically, older age, administration with a meal, and deteriorating renal function result in slower elimination through the kidneys. Fosfomycin crosses the blood-brain barrier, and meningeal inflammation increases its concentration in the CSF. Fosfomycin also penetrates in both cortical and cancellous bone, and penetration correlates with plasma levels and the presence of inflammation.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02654496 | Completed | Obesity |
North Dakota State University |
January 2016 | -- |
| NCT01865812 | Completed | Primary Biliary Cirrhosis |
Intercept Pharmaceuticals |
December 3 2013 | Phase 2 |
| NCT00596427 | Completed | Diabetes |
Carine Beysen|KineMed |
November 2007 | Not Applicable |
| NCT01589523 | Completed | Bile Acid Synthesis Defect|Inborn Error of Bile Acid Metabolism|Inborn Error of Bile Acid Conjugation |
Children''s Hospital Medical Center Cincinnati |
February 2006 | Phase 3 |
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