Original: AFN-1252 620175-39-5, stock more than 100g

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Description: 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.

Name: AFN-1252 

CAS#: 620175-39-5 

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.

IUPAC/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

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).

Harmonized System Code: 293490

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.

6: Flamm RK, Rhomberg PR, Kaplan N, Jones RN, Farrell DJ. Activity of Debio1452, a FabI inhibitor with potent activity against Staphylococcus aureus and coagulase-negative Staphylococcus spp., including multidrug-resistant strains. Antimicrob Agents Chemother. 2015 May;59(5):2583-7. doi: 10.1128/AAC.05119-14. Epub 2015 Feb 17. PubMed PMID: 25691627; PubMed Central PMCID: PMC4394798.

7: Rao KN, Lakshminarasimhan A, Joseph S, Lekshmi SU, Lau MS, Takhi M, Sreenivas K, Nathan S, Yusof R, Abd Rahman N, Ramachandra M, Antony T, Subramanya H. AFN-1252 is a potent inhibitor of enoyl-ACP reductase from Burkholderia pseudomallei--Crystal structure, mode of action, and biological activity. Protein Sci. 2015 May;24(5):832-40. doi: 10.1002/pro.2655. Epub 2015 Apr 2. PubMed PMID: 25644789; PubMed Central PMCID: PMC4420531.

8: Yao J, Abdelrahman YM, Robertson RM, Cox JV, Belland RJ, White SW, Rock CO. Type II fatty acid synthesis is essential for the replication of Chlamydia trachomatis. J Biol Chem. 2014 Aug 8;289(32):22365-76. doi: 10.1074/jbc.M114.584185. Epub 2014 Jun 23. PubMed PMID: 24958721; PubMed Central PMCID: PMC4139244.

9: Yao J, Maxwell JB, Rock CO. Resistance to AFN-1252 arises from missense mutations in Staphylococcus aureus enoyl-acyl carrier protein reductase (FabI). J Biol Chem. 2013 Dec 20;288(51):36261-71. doi: 10.1074/jbc.M113.512905. Epub 2013 Nov 4. PubMed PMID: 24189061; PubMed Central PMCID: PMC3868742.

10: Kaplan N, Garner C, Hafkin B. AFN-1252 in vitro absorption studies and pharmacokinetics following microdosing in healthy subjects. Eur J Pharm Sci. 2013 Nov 20;50(3-4):440-6. doi: 10.1016/j.ejps.2013.08.019. Epub 2013 Aug 27. Erratum in: Eur J Pharm Sci. 2014 Feb 14;52:223. PubMed PMID: 23988847.

11: Parsons JB, Kukula M, Jackson P, Pulse M, Simecka JW, Valtierra D, Weiss WJ, Kaplan N, Rock CO. Perturbation of Staphylococcus aureus gene expression by the enoyl-acyl carrier protein reductase inhibitor AFN-1252. Antimicrob Agents Chemother. 2013 May;57(5):2182-90. doi: 10.1128/AAC.02307-12. Epub 2013 Mar 4. PubMed PMID: 23459481; PubMed Central PMCID: PMC3632907.

12: Tsuji BT, Harigaya Y, Lesse AJ, Forrest A, Ngo D. Activity of AFN-1252, a novel FabI inhibitor, against Staphylococcus aureus in an in vitro pharmacodynamic model simulating human pharmacokinetics. J Chemother. 2013 Feb;25(1):32-5. doi: 10.1179/1973947812Y.0000000060. PubMed PMID: 23433442; PubMed Central PMCID: PMC3558987.

13: Banevicius MA, Kaplan N, Hafkin B, Nicolau DP. Pharmacokinetics, pharmacodynamics and efficacy of novel FabI inhibitor AFN-1252 against MSSA and MRSA in the murine thigh infection model. J Chemother. 2013 Feb;25(1):26-31. doi: 10.1179/1973947812Y.0000000061. PubMed PMID: 23433441; PubMed Central PMCID: PMC3558988.

14: Kaplan N, Awrey D, Bardouniotis E, Berman J, Yethon J, Pauls HW, Hafkin B. In vitro activity (MICs and rate of kill) of AFN-1252, a novel FabI inhibitor, in the presence of serum and in combination with other antibiotics. J Chemother. 2013 Feb;25(1):18-25. doi: 10.1179/1973947812Y.0000000063. PubMed PMID: 23433440; PubMed Central PMCID: PMC3558989.

15: Kaplan N, Albert M, Awrey D, Bardouniotis E, Berman J, Clarke T, Dorsey M, Hafkin B, Ramnauth J, Romanov V, Schmid MB, Thalakada R, Yethon J, Pauls HW. Mode of action, in vitro activity, and in vivo efficacy of AFN-1252, a selective antistaphylococcal FabI inhibitor. Antimicrob Agents Chemother. 2012 Nov;56(11):5865-74. doi: 10.1128/AAC.01411-12. Epub 2012 Sep 4. PubMed PMID: 22948878; PubMed Central PMCID: PMC3486558.

16: Parsons JB, Frank MW, Subramanian C, Saenkham P, Rock CO. Metabolic basis for the differential susceptibility of Gram-positive pathogens to fatty acid synthesis inhibitors. Proc Natl Acad Sci U S A. 2011 Sep 13;108(37):15378-83. doi: 10.1073/pnas.1109208108. Epub 2011 Aug 29. PubMed PMID: 21876172; PubMed Central PMCID: PMC3174620.

17: Karlowsky JA, Kaplan N, Hafkin B, Hoban DJ, Zhanel GG. AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity. Antimicrob Agents Chemother. 2009 Aug;53(8):3544-8. doi: 10.1128/AAC.00400-09. Epub 2009 Jun 1. PubMed PMID: 19487444; PubMed Central PMCID: PMC2715641.

18: Karlowsky JA, Laing NM, Baudry T, Kaplan N, Vaughan D, Hoban DJ, Zhanel GG. In vitro activity of API-1252, a novel FabI inhibitor, against clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis. Antimicrob Agents Chemother. 2007 Apr;51(4):1580-1. Epub 2007 Jan 12. PubMed PMID: 17220418; PubMed Central PMCID: PMC1855524.