AFN-1252

AFN-1252, also known as AFN-12520000; API-1252; Debio-1452, is an enoyl-(acyl-carrier protein) reductase fabl inhibitor potentially for the treatment of acute bacterial skin. AFN-1252 exhibits typical MIC(90) values of ≤0·015 μg/ml against diverse clinical isolates of S. aureus, oral absorption, long elimination half-live and efficacy in animal models. AFN-1252 demonstrates a Staphylococcus-specific spectrum of activity.

Product information

CAS Number: 620175-39-5

Molecular Weight: 375.42

Formula: C22H21N3O3

Synonym:

AFN-12520000

Chemical Name: (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide

Smiles: CC1C2=CC=CC=C2OC=1CN(C)C(=O)/C=C/C1=CN=C2NC(=O)CCC2=C1

InChiKey: QXTWSUQCXCWEHF-JXMROGBWSA-N

InChi: InChI=1S/C22H21N3O3/c1-14-17-5-3-4-6-18(17)28-19(14)13-25(2)21(27)10-7-15-11-16-8-9-20(26)24-22(16)23-12-15/h3-7,10-12H,8-9,13H2,1-2H3,(H,23,24,26)/b10-7+

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Yao J, Ericson ME, Frank MW, Rock CO. Enoyl-Acyl Carrier Protein Reductase I (FabI) is Essential for the Intracellular Growth of Listeria monocytogenes. Infect Immun. 2016 Oct 10. pii: IAI.00647-16. PubMed PMID: 27736774.
2. Hafkin B, Kaplan N, Hunt TL. Safety, tolerability and pharmacokinetics of AFN-1252 administered as immediate release tablets in healthy subjects. Future Microbiol. 2015;10(11):1805-13. doi: 10.2217/fmb.15.101. Epub 2015 Sep 11. PubMed PMID: 26357940.

Products are for research use only. Not for human use.