| Identification | Back Directory | [Name]
L-Tryptophanamide, N2-[(2-mercapto-3-pyridinyl)methyl]-L-ornithyl-L-lysyl-N-[(4'-carboxy-3-mercapto[1,1'-biphenyl]-2-yl)methyl]-N2-methyl-, cyclic (1→3)-thioether | [CAS]
2379336-76-0 | [Synonyms]
Zosurabalpin
L-Tryptophanamide, N2-[(2-mercapto-3-pyridinyl)methyl]-L-ornithyl-L-lysyl-N-[(4'-carboxy-3-mercapto[1,1'-biphenyl]-2-yl)methyl]-N2-methyl-, cyclic (1→3)-thioether | [Molecular Formula]
C43H50N8O5S | [MOL File]
2379336-76-0.mol | [Molecular Weight]
790.98 |
| Chemical Properties | Back Directory | [Boiling point ]
1108.0±65.0 °C(Predicted) | [density ]
1.229±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
4.06±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Zosurabalpin is a polypeptide antibiotic targeting LPS transporter (LptB2FGC complex), which can block the transport of LPS and lead to endotoxin accumulation in cells, and has shown excellent antibacterial activity against Carbapenem-resistant Acinetobacter baumanni (CRAB) [1] [2]. | [in vivo]
Zosurabalpin (6-360?mg/kg/day; subcutaneous injection; every 6 h for 24 h) exerts antibacterial activity in neutropaenic mouse thigh and lung infection model [3]. | Animal Model: | Cyclophosphamide monohydrate (HY-17420A) and bacterial suspension treaded male CD-1 mice [3] | | Dosage: | 6-360?mg/kg/day | | Administration: | Subcutaneous injection (s.c.), every 6?h for 24 h | | Result: | Decreased in bacterial burden in a dose-dependent manner.
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| [References]
[1] Weng Q, et al. Zosurabalpin: a novel tethered macrocyclic peptide antibiotic that kills carbapenem-resistant Acinetobacter baumannii. MedComm (2020). 2024 Aug 11;5(8):e696. DOI:10.1002/mco2.696
[2] Skudlarek JW, et al. Cerastecin Inhibition of the Lipooligosaccharide Transporter MsbA to Combat Acinetobacter baumannii: From Screening Impurity to In Vivo Efficacy. J Med Chem. 2024 Sep 12;67(17):15620-15675. DOI:10.1021/acs.jmedchem.4c01277
[3] Zampaloni C, et al. A novel antibiotic class targeting the lipopolysaccharide transporter. Nature. 2024 Jan;625(7995):566-571. doi: 10.1038/s41586-023-06873-0. Epub 2024 Jan 3. Erratum in: Nature. 2024 Jul;631(8022):E17. DOI:10.1038/s41586-023-06873-0
[4] Hawser, S, et al. 2131. Activity of the Novel Antibiotic Zosurabalpin (RG6006) against Clinical Acinetobacter Isolates from China. Open Forum Infect Dis 2023, 10, ofad500.1754. |
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