AFN-1252

Cas：620175-39-5

Product Information：

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.

Chemical Formula: C22H21N3O3

Exact Mass: 375.1583

Molecular Weight: 375.428

Elemental Analysis: C, 70.38; H, 5.64; N, 11.19; O, 12.78

Synonym:

AFN-1252

AFN 1252

AFN1252

AFN-12520000

API-1252

Debio-1452

AFN12520000

API1252

Debio1452

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

InChi Key:

QXTWSUQCXCWEHF-JXMROGBWSA-N

InChi Code: 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+

Smiles Code:

O=C(N(C)CC1=C(C)C2=CC=CC=C2O1)/C=C/C3=CC(CC4)=C(N=C3)NC4=O

Technical Data：

Appearance: White to off-white solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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, Murphy B. Efficacy and Safety of AFN-1252, the First Staphylococcus-Specific Antibacterial Agent, in the Treatment of Acute Bacterial Skin and Skin Structure Infections, Including Those in Patients with Significant Comorbidities. Antimicrob Agents Chemother. 2015 Dec 28;60(3):1695-701. doi: 10.1128/AAC.01741-15. PubMed PMID: 26711777; PubMed Central PMCID: PMC4775962.

3. Yao J, Bruhn DF, Frank MW, Lee RE, Rock CO. Activation of Exogenous Fatty Acids to Acyl-Acyl Carrier Protein Cannot Bypass FabI Inhibition in Neisseria. J Biol Chem. 2016 Jan 1;291(1):171-81. doi: 10.1074/jbc.M115.699462. Epub 2015 Nov 13. PubMed PMID: 26567338; PubMed Central PMCID: PMC4697154.

4. Hunt T, Kaplan N, Hafkin B. Safety, tolerability and pharmacokinetics of multiple oral doses of AFN-1252 administered as immediate release (IR) tablets in healthy subjects. J Chemother. 2016 Jun;28(3):164-71. doi: 10.1179/1973947815Y.0000000075. Epub 2016 May 13. PubMed PMID: 26431470.

5. 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.