AFN-1252
- Product Name
- AFN-1252
- CAS No.
- 620175-39-5
- Chemical Name
- AFN-1252
- Synonyms
- CS-2098;AFN-1252;Debio-1452;AFN-1252, API-1252;Debio-1452(AFN1252);AFN-1252(Debio 1452);API1252; DEBIO1452;API 1252; DEBIO-1452;API1252; DEBIO1452;Antibiotic,AFN 1252,AFN1252,inhibit,API1252,Bacterial,Debio-1452,AFN-1252,Debio1452,Inhibitor,API 1252;(E)-N-Methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide;(E)-3-(1,2,3,4-tetrahydro-2-oxo-1,8-naphthyridin-6-yl)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)acrylamide
- CBNumber
- CB23041381
- Molecular Formula
- C22H21N3O3
- Formula Weight
- 375.42
- MOL File
- 620175-39-5.mol
AFN-1252 Property
- Boiling point:
- 601.2±65.0 °C(Predicted)
- Density
- 1.28±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO:5.8(Max Conc. mg/mL);15.45(Max Conc. mM)
- form
- A crystalline solid
- pka
- 3.60±0.20(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 24686
- Product name
- AFN-1252
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 24686
- Product name
- AFN-1252
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $270
- Updated
- 2024/03/01
- Product number
- 24686
- Product name
- AFN-1252
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $507
- Updated
- 2024/03/01
- Product number
- 24686
- Product name
- AFN-1252
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $1189
- Updated
- 2024/03/01
- Product number
- A425005
- Product name
- AFN-1252
- Packaging
- 5mg
- Price
- $285
- Updated
- 2021/12/16
AFN-1252 Chemical Properties,Usage,Production
Description
AFN-1252 is an inhibitor of staphylococcal enoyl-acyl carrier protein reductase (FabI; Ki = 12.8 nM), an enzyme that activates bacterial fatty acid biosynthesis. It is selective for isolates of methicillin-susceptible and methicillin-resistant S. aureus (MIC90s = ≤0.008 μg/ml) over isolates of S. pneumoniae, β-hemolytic streptococci, Enterococcus, Enterobacteriaceae, non-fermentative Gram-negative bacilli, and M. catarrhalis (MIC90s = >4 μg/ml). In vivo, AFN-1252 increases survival in a murine acute lethal septicemia model, showing 100% survival when administered at a single oral dose of 1 mg/kg.
Uses
AFN-1252 is a staphylococcus-selective enoyl-acyl carrier protein reductase (FabI) inhibitor. An antimicrobial agent
Enzyme inhibitor
This selective, orally available, first-in-class antibiotic (FW = 375.43 g/mol; CAS 620175-39-5; Formulated in 1% Poloxamer 407) is a potent inhibitor of Staphylococcus aureus enoyl-acyl carrier protein reductase (FabI), thereby preventing fatty acyl chain elongation and disrupting biosynthesis of both saturated and unsaturated fatty acids needed for bacterial growth. It demonstrates exceptional potency and specificity against staphylococcal isolates, with typical S. aureus MIC ranges of 0.002–0.12 μg/mL and MIC90s of ≤ 0.015 μg/mL. Mode of Action: FabI is the only enoyl-ACP reductase in S. aureus, S. epidermidis, and related staphylococci, with no alternative enzyme or rescue pathway, including processing of exogenously supplied fatty acids. Such metabolic features suggest FabI may be essential to cell viability in Staphylococcus spp. The inhibitor’s target was convincingly confirmed (a) by using direct enzyme assays (IC50 = 14 nM, with no inhibition of the human enzyme, even at 67 μM); (b) by employing radiolabeled acetate to demonstrate that AFN-1252 greatly reduced incorporation into lipids; (c) by co-crystallizing AFN-1252 and FabI in the presence of the unnatural substrate 3′-NADPH, and (d) by genetically determining AFN-1252’s spontaneous resistance frequency and characterizing AFN-1252-resistant FabI mutants. In socalled time-kill assays, AFN-1252 caused a time-dependent reduction in the viability of S. aureus ATCC 29213 (MSSA) and S. aureus ATCC 43300 (MRSA), with similar magnitudes and rates of killing were obtained at 4 and 128 times the MIC (i.e., 2.0- and 2.9-log10 reductions).
AFN-1252 Preparation Products And Raw materials
Raw materials
Preparation Products
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