产品描述
Taniborbactam hydrochloride is a reversible and selective inhibitor of boronic acid-containing pan-spectrum β-lactamase(IC50s of 8-530 nM).
体外活性
Taniborbactam hydrochloride (VNRX-5133 hydrochloride) (IC50s of 0.5 nM, 2 nM, 0.5 nM, 0.06 nM for KPC-2, OXA-48, VIM-4 of K.pneumoniae strain and VIM-2 of P.aeruginosa strain)[2]. Both cefepime/Taniborbactam hydrochloride (10 μg/mL) and meropenem/Taniborbactam hydrochloride combinations are highly active against all six of the NDM-1-producing clinical isolates from K.pneumoniae and E.coli(MIC ranges of 16-0.25 and 1-0.125 μg/mL, respectively)[1].
体内活性
In the neutropenic mouse lung infection model, A single dose of cefepime (32 mg/kg)/Taniborbactam hydrochloride (VNRX-5133 hydrochloride; 16 mg/kg; s.c.) achieves >4 log10 reduction in viable bacterial counts against a CTX-M-14-producing strain of K.pneumoniae[2]. Combination of Cefepime (16 mg/kg) and Taniborbactam hydrochloride (16 mg/kg; s.c.; twice-a-day for 7 days) demonstrates >2 log10 reductions in viable bacterial counts in the kidney of the ascending urinary tract infection model against a CTX-M-15-producing strain of E.coli[2]. Taniborbactam hydrochloride has a T1/2 of 0.16 hours, a CL of 618 mL/h/kg, and a Vss of 143 mL/kg for mice[2].
Cas No.
2244235-49-0
分子式
C19H30BCl2N3O5
分子量
462.18
别名
VNRX-5133 hydrochloride;Taniborbactam hydrochloride
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years