[CAS NO. 1802363-75-2]  Metallo-β-lactamase-IN-9

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PRODUCTS SPECIFICATIONS [1802363-75-2]

Catalog
HY-152105
Brand
MCE
CAS
1802363-75-2

DESCRIPTION [1802363-75-2]

Overview

MDL-
Molecular Weight332.34
Molecular FormulaC13H12N6O3S
SMILESOCC1=CC=C(C=C1)C2=CC=NC(S(=O)(N)=O)=C2C3=NN=NN3

For research use only. We do not sell to patients.

Summary

Metallo-β-lactamase-IN-9 (Compound 23) is a pan metallo-beta-lactamase ( MBL ) inhibitor with IC 50 s of 35, 269 and 369 nM against NDM-1 , VIM-1 and IMP-1 , respectively [1] .


IC50 & Target

IC50: 35 nM (NDM-1), 269 nM (VIM-1), 369 nM (IMP-1) [1]


In Vivo

Metallo-β-lactamase-IN-9 (Compound 23) (10 and 50 mg/kg; s.c.; three times a day for 1 day) reduces bacterial burden in both the spleen and kidney in combination with Imipenem (HY-B1369A) in a Klebsiella pneumoniae MB9249 infection mice model [1] .
Mouse Pharmacokinetic Properties of Metallo-β-lactamase-IN-9 (Compound 23) d [1]

dose a (iv, mpk) AUC (μM·h) MRT (h) V dss (L/kg) Cl (mL/min/kg)
5 a 27.08 5.2 2.97 9.33

dose (sc, mg/kg) AUC (μM·h) C max (μM) T max (h)
10 b 27.42 13.4 0.83
50 c 111.28 69.1 0.5

a Formulation, 1.0 mg/mL 23 in 20% DMSO/60% PEG400/20% water (solution) with dose volume of 5 mL/kg.
b Formulation, 1.0 mg/mL of 23 in 30% captisol (solution) with dose volume 10 mL/kg.
c Formulation, 5.0 mg/mL of 23 in 30% captisol (solution) with dose volume of 10 mL/kg.
d AUC, area under the curve; Cl, clearance; iv, intravenous, MRT, mean residence time; V dss , volume of distribution at steady state.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cytoxan-treated DBA-2 mice, Klebsiella pneumoniae MB9249 infection model [1]
Dosage: 10 and 50 mg/kg, in combination with 5mg/kg Imipenem (HY-B1369A)
Administration: Subcutaneous injection, three times a day for 1 day
Result: Demonstrated reduction of bacterial burden in both the spleen and kidney to a greater extent while combining with Imipenem (HY-B1369A) relative to Imipenem (HY-B1369A) alone.
Animal Model: C57BL/6 mice [1]
Dosage: Intravenous and subcutaneous injection
Administration: 5, 10 and 50 mg/kg (Pharmacokinetic Analysis)
Result: Showed good pharmacokinetic properties.

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.