Metallo-β-lactamase-IN-6_product_DataBase

Bioactivity	Metallo-β-lactamase-IN-6 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.56 μM, 29.50 μM and 5.78 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-6 displays potent synergistic antibacterial activity with Meropenem against engineered Escherichia coli strains and intractable clinically isolated Pseudomonas aeruginosa producing VIM-2 MBL[1].
Target	IC50: 0.56 μM (VIM-2), 29.50 μM (VIM-1), 5.78 μM (VIM-5)
Invitro	Metallo-β-lactamase-IN-6 (compound 55) (10 μM; 18 - 20 hours) can potentiate Meropenem activity against VIM-2 mediated antibacterial resistance with FIC index values of 0.05[1].Metallo-β-lactamase-IN-6 (1, 10, 100 μM; 18 - 20 hours) can penetrate E. coli outer membrane and restore Meropenem activity against PBP3 by blocking destructive effect of VIM-2 enzyme to Meropenem[1].Metallo-β-lactamase-IN-6 (100 μM) potentiates the antibacterial activity of Meropenem against PA W35 with FIC index values of 0.25[1].
In Vivo	Metallo-β-lactamase-IN-6 (100 mg/kg; IP; single) reaches plasma concentration peak about 9 min after injection with an effective maximum concentration of 142.8 μg/ml, and the T1/2 is 1.24 hours[1].Metallo-β-lactamase-IN-6 (500, 1000, or 2000 mg/kg; IP; single, observe for 14 days) does not result in any significant toxic effects and is well-tolerated by mice at a dose of ≤ 2000 mg/kg[1].Pharmacokinetic Parameters of Metallo-β-lactamase-IN-6 in male female ICR mice[1].
Name	Metallo-β-lactamase-IN-6
CAS	1439899-44-1
Formula	C10H9N3O2
Molar Mass	203.20
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Yan YH, Li W, Chen W, et al. Structure-guided optimization of 1H-imidazole-2-carboxylic acid derivatives affording potent VIM-Type metallo-β-lactamase inhibitors. Eur J Med Chem. 2022;228:113965.

PeptideDB

Metallo-β-lactamase-IN-6

CAS: 1439899-44-1 F: C10H9N3O2 W: 203.20