Taniborbactam hydrochloride (VNRX-5133 hydrochloride) 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 hydrochloride 对 KPC-2，AmpC，OXA-48 和 VIM-2 的 IC₅₀ 分别为 30 nM，32 nM，42 nM，20 nM。Taniborbactam hydrochloride 具有抗革兰氏阴性菌 (bacteria) 活性。

Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC 50 s of 8-530 nM. Taniborbactam hydrochloride has IC 50 s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam hydrochloride is against Gram-negative bacteria.

Solid

β-lactamase

Taniborbactam hydrochloride (VNRX-5133 hydrochloride) 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 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 , with MIC ranges of 16-0.25 and 1-0.125 μg/mL, respectively.
has not independently confirmed the accuracy of these methods. They are for reference only.

A single dose of cefepime (32 mg/kg)/Taniborbactam hydrochloride (VNRX-5133 hydrochloride; 16 mg/kg; s.c.) achieves >4 log 10 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 hydrochloride (16 mg/kg; s.c.; twice-a-day for 7 days) demonstrates >2 log 10 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 hydrochloride has a T 1/2 of 0.16 hours, a CL of 618 mL/h/kg, and a V ss of 143 mL/kg for mice.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

[1]. Krajnc A, et al. Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. J Med Chem. 2019 Sep 26;62(18):8544-8556.
[2]. Liu B ,et al. Discovery of Taniborbactam (VNRX-5133): A Broad-Spectrum Serine- and Metallo-β-lactamase Inhibitor for Carbapenem-Resistant Bacterial Infections. J Med Chem. 2019 Dec 16.

In Vitro: DMSO : 200 mg/mL (432.73 mM; Need ultrasonic)H₂O : 33.33 mg/mL (72.11 mM; Need ultrasonic)配制储备液