AN0128

AN0128, also known as CRM-0005 and ONT-0001, is a tumour necrosis factor alpha (TNF-α) inhibitor potentially for the treatment of atopic dermatitis. AN0128 showed promising combination of anti-bacterial and anti-inflammatory activities. This compound is now in clinical development for dermatological conditions. Daily application of AN0128 (1%) compared with controls reduced bone loss by 38 to 44% (P < 0.05), while vehicle alone had no effect (P > 0.05). The reduction in bone loss with AN0128 was similar to that achieved with a NSAID, ketorolac, and Total toothpaste containing triclosan. AN0128 also reduced the level of gingival inflammation 42% compared with the ligature only (P < 0.05), whereas vehicle alone had no effect (P > 0.05). The results indicate that AN0128 significantly reduces the formation of an inflammatory infiltrate and reduces bone loss, measured histologically and by micro-CT.

Product information

CAS Number: 872044-70-7

Molecular Weight: 400.06

Formula: C20H16BCl2NO3

Chemical Name: ((bis(3-chloro-4-methylphenyl)boraneyl)oxy)(3-hydroxypyridin-2-yl)methanone

Smiles: CC1C=CC(=CC=1Cl)B(OC(=O)C1=NC=CC=C1O)C1C=C(Cl)C(C)=CC=1

InChiKey: ZTLSOLUCMQEGEA-UHFFFAOYSA-N

InChi: InChI=1S/C20H16BCl2NO3/c1-12-5-7-14(10-16(12)22)21(15-8-6-13(2)17(23)11-15)27-20(26)19-18(25)4-3-9-24-19/h3-11,25H,1-2H3

Technical Data

Appearance: Solid Power

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

Solubility: To be determined

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: ≥12 months 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. Baker SJ, Akama T, Zhang YK, Sauro V, Pandit C, Singh R, Kully M, Khan J, Plattner JJ, Benkovic SJ, Lee V, Maples KR. 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. PubMed PMID: 16997550.
2. Luan Q, Desta T, Chehab L, Sanders VJ, Plattner J, Graves DT. Inhibition of experimental periodontitis by a topical boron-based antimicrobial. J Dent Res. 2008 Feb;87(2):148-52. PubMed PMID: 18218841.

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