产品描述
Taniborbactam is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor (IC50s: 8-530 nM). Taniborbactam has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2.
体外活性
Both cefepime/Taniborbactam (10 μg/mL) and meropenem/Taniborbactam 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). Taniborbactam has 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 [1][2].
体内活性
Taniborbactam has a T1/2 of 0.16 hours, a CL of 618 mL/h/kg, and a Vss of 143 mL/kg for mice. Combination of Cefepime (16 mg/kg) and Taniborbactam (16 mg/kg; s.c.; twice-a-day for 7 days) shows >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. A single dose of cefepime (32 mg/kg)/Taniborbactam (16 mg/kg; s.c.) achieves >4 log10 reductions in viable bacterial counts in the neutropenic mouse lung infection model against a CTX-M-14-producing strain of K.pneumoniae [2].
Cas No.
1613267-49-4
分子式
C19H28BN3O5
分子量
389.25
别名
VNRX-5133
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