For research use only. Not for therapeutic Use.
Acoziborole（Cat No.:I001122）is an innovative oral medication developed to treat human African trypanosomiasis (HAT), also known as sleeping sickness, caused by Trypanosoma brucei parasites. It works by inhibiting an enzyme critical for the parasite’s survival, leading to rapid parasite death. Acoziborole’s single-dose regimen is a breakthrough, especially for remote regions where multi-dose treatments are challenging. With efficacy in both early and late stages of HAT, it offers a simpler, safer alternative to existing treatments, potentially transforming HAT control efforts and reducing the disease burden in endemic areas across sub-Saharan Africa.
| Catalog Number | I001122 |
| CAS Number | 1266084-51-8 |
| Synonyms | SCYX-7158; SCYX7158; SCYX 7158; Oxaborole; Acoziborole.;4-fluoro-N-(1-hydroxy-3,3-dimethyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)-2-(trifluoromethyl)benzamide |
| Molecular Formula | C17H14BF4NO3 |
| Purity | ≥95% |
| Solubility | Soluble in DMSO |
| Storage | 0 - 4°C for short term (days to weeks), or -20 °C for long term (months). |
| IUPAC Name | 4-fluoro-N-(1-hydroxy-3,3-dimethyl-2,1-benzoxaborol-6-yl)-2-(trifluoromethyl)benzamide |
| InChI | InChI=1S/C17H14BF4NO3/c1-16(2)12-6-4-10(8-14(12)18(25)26-16)23-15(24)11-5-3-9(19)7-13(11)17(20,21)22/h3-8,25H,1-2H3,(H,23,24) |
| InChIKey | PTYGDEXEGLDNAZ-UHFFFAOYSA-N |
| SMILES | B1(C2=C(C=CC(=C2)NC(=O)C3=C(C=C(C=C3)F)C(F)(F)F)C(O1)(C)C)O |
| Reference | </br>1: Li X, Zhang YK, Plattner JJ, Mao W, Alley MR, Xia Y, Hernandez V, Zhou Y, Ding</br> CZ, Li J, Shao Z, Zhang H, Xu M. Synthesis and antibacterial evaluation of a</br> novel tricyclic oxaborole-fused fluoroquinolone. Bioorg Med Chem Lett. 2013 Feb</br> 15;23(4):963-6. doi: 10.1016/j.bmcl.2012.12.045. Epub 2012 Dec 21. PubMed PMID:</br> 23312945.</br>2: Shapiro AB, Gao N, Hajec L, McKinney DC. Time-dependent, reversible, oxaborole</br> inhibition of Escherichia coli leucyl-tRNA synthetase measured with a continuous </br> fluorescence assay. Anal Biochem. 2012 Dec 1;431(1):48-53. doi:</br> 10.1016/j.ab.2012.08.024. Epub 2012 Sep 10. PubMed PMID: 22975201.</br>3: Nare B, Wring S, Bacchi C, Beaudet B, Bowling T, Brun R, Chen D, Ding C,</br> Freund Y, Gaukel E, Hussain A, Jarnagin K, Jenks M, Kaiser M, Mercer L, Mejia E, </br> Noe A, Orr M, Parham R, Plattner J, Randolph R, Rattendi D, Rewerts C, Sligar J, </br> Yarlett N, Don R, Jacobs R. Discovery of novel orally bioavailable oxaborole</br> 6-carboxamides that demonstrate cure in a murine model of late-stage central</br> nervous system african trypanosomiasis. Antimicrob Agents Chemother. 2010</br> Oct;54(10):4379-88. doi: 10.1128/AAC.00498-10. Epub 2010 Jul 26. PubMed PMID:</br> 20660666; PubMed Central PMCID: PMC2944573.</br>4: Hui X, Baker SJ, Wester RC, Barbadillo S, Cashmore AK, Sanders V, Hold KM,</br> Akama T, Zhang YK, Plattner JJ, Maibach HI. In Vitro penetration of a novel</br> oxaborole antifungal (AN2690) into the human nail plate. J Pharm Sci. 2007</br> Oct;96(10):2622-31. PubMed PMID: 17621679.</br></br> |
