Metallo-β-lactamase-IN-6
Modify Date: 2024-01-27 20:07:51
Metallo-β-lactamase-IN-6 structure
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Common Name | Metallo-β-lactamase-IN-6 | ||
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| CAS Number | 1439899-44-1 | Molecular Weight | 203.20 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C10H9N3O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Metallo-β-lactamase-IN-6Metallo-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]. |
| Name | Metallo-β-lactamase-IN-6 |
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| Description | 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]. |
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| Related Catalog | |
| Target |
IC50: 0.56 μM (VIM-2), 29.50 μM (VIM-1), 5.78 μM (VIM-5)[1] |
| In Vitro | 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]. IP (100 mg/kg) T1/2 (h) 1.243 Cmax (μg/mL) 142.8 Tmax (h) 0.151 Vd (mL/kg) 535.804 CL (mL/h/kg) 248.512 AUC0-∞ (μg/mL·h) 896 Animal Model: Female ICR mice (180-220 g)[1] Dosage: 100 mg/kg Administration: IP; single (Pharmacokinetics Analysis) Result: Plasma concentration reached its peak about 9 min after injection with an effective maximum concentration of 142.8 μg/ml, and the T1/2 was 1.24 hours. Animal Model: Female ICR mice (n=5)[1] Dosage: 500, 1000, or 2000 mg/kg Administration: IP; single, observed for 14 days Result: Did not result in any significant toxic effects and was well-tolerated by mice at a dose of ≤ 2000 mg/kg. |
| References |
| Molecular Formula | C10H9N3O2 |
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| Molecular Weight | 203.20 |