In Vitro |
ANT3310 sodium (Compound 21, 0.006 to 3 000 nM, 10 min) inhibits a series of Serine β-Lactamase (AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2), with IC<>50 values ranging from 1 nM to 175 nM[1]. ANT3310 sodium shows a low in vitro cytotoxicity (IC<>50: > 100 μM) in HepG2 cell, cardiotoxicity (inhibition of the hERG potassium ion channel), and genotoxicity (Ames test)[1].
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In Vivo |
ANT3310 sodium (intravenous injection, 25-100 mg/kg, at 1, 3, 5, and 7 h postinfection) reduces bacterial burdens in murine thigh infection model[1]. ANT3310 sodium (intravenous injection, 1 mg/kg, Male Swiss albino mice) shows a T1/2 value of 0.64 h, AUC value of 412 ng•h/mL, and Cl value of 40 mL/min/kg (pharmacokinetic assay)[1]. Animal Model: Murine thigh infection model[1] Dosage: 25, 50, and 100 mg/kg Administration: Intravenous injection, at 1, 3, 5, and 7 h postinfection Result: Reduced bacterial burdens (colony forming units, CFU) in a dose-dependent manner to levels below that of the initial starting inoculum at the highest dose, when treated with the combination of MEM.
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