Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Metallo-β-lactamase-IN-9 (Compound 23) serves as a broad-spectrum inhibitor of metallo-beta-lactamases (MBL), exhibiting inhibition constants (IC50) of 35 nM for NDM-1, 269 nM for VIM-1, and 369 nM for IMP-1 [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | Metallo-β-lactamase-IN-9 (Compound 23) serves as a broad-spectrum inhibitor of metallo-beta-lactamases (MBL), exhibiting inhibition constants (IC50) of 35 nM for NDM-1, 269 nM for VIM-1, and 369 nM for IMP-1 [1]. |
In vivo | Metallo-β-lactamase-IN-9 (Compound 23) co-administered with Imipenem at doses of 10 and 50 mg/kg, subcutaneously injected three times daily for a day, reduced the bacterial load in the spleens and kidneys in a mouse Klebsiella pneumoniae MB9249 infection model [1]. The pharmacokinetic profile of Metallo-β-lactamase-IN-9 (Compound 23) in mice revealed the following after a single dose: intravenous administration (1 mg/kg) resulted in an area under the curve (AUC) of 27.08 μM·h, mean residence time (MRT) of 5.2 hours, steady-state volume of distribution (Vdss) of 2.97 L/kg, and a clearance rate (Cl) of 9.33 mL/min/kg. Subcutaneous dosing showed an AUC of 27.42 μM·h at 10 mg/kg and 111.28 μM·h at 50 mg/kg, with Cmax values of 13.4 and 69.1 μM and Tmax of 0.83 and 0.5 hours, respectively. Formulations included a 1.0 mg/mL concentration of Compound 23 in 20% DMSO/60% PEG400/20% water at a 5 mL/kg dose volume for intravenous delivery and 1.0 mg/mL or 5.0 mg/mL concentrations in 30% captisol for subcutaneous injection at 10 mL/kg dose volume [1]. |
Molecular Weight | 332.34 |
Formula | C13H12N6O3S |
CAS No. | 1802363-75-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Metallo-β-lactamase-IN-9 1802363-75-2 inhibitor inhibit