Taniborbactam

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Taniborbactam 是一种新型 β-内酰胺酶抑制剂，用于治疗细菌感染。

Taniborbactam is a novel beta-lactamase inhibitor for the treatment of bacterial infections.

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.

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.

Taniborbactam

GPCR/G Protein

Antibacterial

Antibacterial

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1613267-49-4

389.259

C19H28BN3O5

>98% (HPLC)

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O=C(C1=C(OB(O)[C@@H](NC(C[C@H]2CC[C@H](NCCN)CC2)=O)C3)C3=CC=C1)O

(3R)-3-(2-{trans-4-[(2-aminoethyl)amino]cyclohexyl}acetamido)-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid

(-20℃)

With Ice Pack

≥ 2 years