Taniborbactam (Synonyms:VNRX-5133)
目录号 : KM7975 CAS No. : 1613267-49-4

Taniborbactam (VNRX-5133) 是一种可逆的,选择性的含硼酸全光谱 β-内酰胺酶 (β-lactamase) 抑制剂,IC50 为 8-530 nM。Taniborbactam 对 KPC-2,AmpC,OXA-48 和 VIM-2 的 IC50 分别为 30 nM,32 nM,42 nM,20 nM。Taniborbactam 具有抗革兰氏阴性菌 (bacteria) 活性。

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5mg
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10mg
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50mg
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生物活性

Taniborbactam (VNRX-5133) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam is against Gram-negative bacteria.

体外研究

Taniborbactam (VNRX-5133) 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.
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, with MIC ranges of 16-0.25 and 1-0.125 μg/mL, respectively.

体内研究

A single dose of cefepime (32 mg/kg)/Taniborbactam (VNRX-5133; 16 mg/kg; s.c.) achieves >4 log10 reduction in viable bacterial counts in the neutropenic mouse lung infection model against a CTX-M-14-producing strain of K.pneumoniae.
Combination of Cefepime (16 mg/kg) and Taniborbactam (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.
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.

分子式
C19H28BN3O5
分子量
389.25
CAS号
1613267-49-4
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

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科研文献
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