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AN0128

Names

[ CAS No. ]:
872044-70-7

[ Name ]:
AN0128

[Synonym ]:
2-Pyridinecarboxylic acid, 3-hydroxy-, anhydride with bis(3-chloro-4-methylphenyl)borinic acid

Biological Activity

[Description]:

AN0128 is a boron-containing antibacterial and anti-inflammatory agent. AN0128 against S. aureus, S. epidermidis, P. acnes, B. subtilis with minimum inhibitory concentration (MIC) values of 1, 0.5, 0.3, 1 μg/mL. AN0128 can be used for the research of periodontal disease and cutaneous diseases[1][2].

[Related Catalog]:

Research Areas >> Infection
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

AN0128 (compound 2g; 10 μM; 24-48 hours) shows strong inhibition of the release of pro-inflammatory cytokines (TNF-α, IL-1β) but no inhibition of IFN-γ or IL-4 release in human peripheral blood mononuclear cells (PBMCs)[1].

[In Vivo]

AN0128 (1%, 5%; daily topical daub for 7 days) significantly reduces the formation of an inflammatory infiltrate and reduces bone loss[2]. Animal Model: Experimental periodontitis in twelve-week-old male Sprague-Dawley rats (weighing from 275 to 300 g each)[2] Dosage: 1% AN0128 in 40% Transcutol P, 40% PBS, and 20% ethanol vehicle Administration: Daily topical daub for 7 days Result: Similar to Ketorolac, resulting 50% and 35% increase in bone area and bone volume respectively, and 38%, 42% decrease in bone loss and inflammation respectively. Animal Model: Experimental periodontitis in twelve-week-old male Sprague-Dawley rats (weighing from 275 to 300 g each)[2] Dosage: 5% with Total toothpaste Administration: Applied daily via a cotton-tip applicator. for 7 days Result: Had more effect than Total toothpaste, resulting in a 33% increase in bone volume, and a 47% decrease in bone loss.

[References]

[1]. Baker SJ, et al. Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases. Bioorg Med Chem Lett. 2006 Dec 1;16(23):5963-7.

[2]. Luan Q, et al. Inhibition of experimental periodontitis by a topical boron-based antimicrobial. J Dent Res. 2008 Feb;87(2):148-52.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H16BCl2NO3

[ Molecular Weight ]:
400.06300

[ Exact Mass ]:
399.06000

[ PSA ]:
59.42000

[ LogP ]:
3.67350


Related Compounds