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.

Product information

CAS Number: 1613267-49-4

Molecular Weight: 389.25

Formula: C19H28BN3O5

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

Smiles: NCCN[C@@H]1CC[C@@H](CC(=O)N[C@H]2CC3=CC=CC(=C3OB2O)C(O)=O)CC1

InChiKey: PFZUWUXKQPRWAL-NOLJZWGESA-N

InChi: InChI=1S/C19H28BN3O5/c21-8-9-22-14-6-4-12(5-7-14)10-17(24)23-16-11-13-2-1-3-15(19(25)26)18(13)28-20(16)27/h1-3,12,14,16,22,27H,4-11,21H2,(H,23,24)(H,25,26)/t12-,14-,16-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

In Vivo:

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.

Products are for research use only. Not for human use.