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AFN-1252

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Catalog No. T4105Cas No. 620175-39-5
Alias Debio 1452, API-1252

AFN-1252 (Debio 1452)(Debio 1452) is an effective inhibitor of enoyl-acyl carrier protein reductase (FabI). It (≤0.12 μg/ml) inhibits all Clinicalal isolates of Staphylococcus aureus and Staphylococcus epidermidis.

AFN-1252

AFN-1252

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Purity: 99.81%
Catalog No. T4105Alias Debio 1452, API-1252Cas No. 620175-39-5
AFN-1252 (Debio 1452)(Debio 1452) is an effective inhibitor of enoyl-acyl carrier protein reductase (FabI). It (≤0.12 μg/ml) inhibits all Clinicalal isolates of Staphylococcus aureus and Staphylococcus epidermidis.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$40In StockIn Stock
2 mg$59In StockIn Stock
5 mg$97In StockIn Stock
10 mg$155In StockIn Stock
25 mg$289In StockIn Stock
50 mg$443In StockIn Stock
100 mg$653In StockIn Stock
1 mL x 10 mM (in DMSO)$97In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.81%
Color:White
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Product Introduction

AFN-1252 AI Summary
AFN-1252 demonstrates potent antibacterial activity, particularly against methicillin-susceptible and methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, with MIC50 values of <= 0.008 µg/mL. It also exhibits moderate antibacterial activity against Streptococcus pyogenes, Enterococcus faecium, and some strains of Escherichia coli and Klebsiella pneumoniae, with MIC values ranging from 0.5 to 4.0 µg/mL. However, the compound shows limited activity against Streptococcus pneumoniae and Stenotrophomonas maltophilia, with MIC values exceeding 4.0 µg/mL. The compound has a LogD7.4 value of 2.36 and a high plasma protein binding percentage of 94.56%, suggesting significant distribution in biological systems. In terms of bioactivity, AFN-1252 effectively inhibits the Staphylococcus aureus FabI enzyme, with an IC50 value of 29.0 nM. It maintains metabolic stability in mouse liver microsomes and has acceptable pharmacokinetic parameters in Swiss albino CD-1 mice, including a half-life of 1.84 hours and an AUC of 2200.0 ng·hr/mL at an oral dose of 10 mg/kg. The compound is also highly protein-bound in mouse, rat, dog, and human serum, with a binding percentage of 95.0%. Additionally, AFN-1252 exhibits antiviral properties, notably against SARS-CoV-2, by inhibiting virus-induced cytotoxicity in VERO-6 and Caco-2 cells and shows inhibition of the SARS-CoV-2 3CL-Pro protease. It presents a significant inhibitory effect (77.06%) on human HDAC6 using a commercial peptide substrate, although its inhibitory effect varies with different substrates. Overall, AFN-1252 shows promise as a potent antibacterial and antiviral agent with substantial bioactivity against key bacterial enzymes and viral proteases..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
AFN-1252 (Debio 1452)(Debio 1452) is an effective inhibitor of enoyl-acyl carrier protein reductase (FabI). It (≤0.12 μg/ml) inhibits all Clinicalal isolates of Staphylococcus aureus and Staphylococcus epidermidis.
SynonymsDebio 1452, API-1252
Chemical Properties
Molecular Weight375.42
FormulaC22H21N3O3
Cas No.620175-39-5
SmilesCN(Cc1oc2ccccc2c1C)C(=O)\C=C\C1=CNC2=NC(=O)CCC2=C1
Relative Density.1.28 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 5.8 mg/mL (15.45 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6637 mL13.3184 mL26.6368 mL133.1842 mL
5 mM0.5327 mL2.6637 mL5.3274 mL26.6368 mL
10 mM0.2664 mL1.3318 mL2.6637 mL13.3184 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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