Taniborbactam  (Synonyms: VNRX-5133)

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^[1][2].

β-lactamase^[1]

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^[2].
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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].
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^[2].
Taniborbactam 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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

389.25

C₁₉H₂₈BN₃O₅

1613267-49-4

Solid

White to off-white

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

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)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [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.  [Content Brief]