Taniborbactam hydrochloride (C007B-431310)

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 bacteriaIn VitroTaniborbactam hydrochloride (VNRX-5133 hydrochloride) has IC 50 s 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. ?/nBoth 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoA single dose of Cefepime (HY-B0692) (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. ?/nCombination 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. ?/nTaniborbactam 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:β-lactamase. Specification: 0.99 Molecular Formula: C19H30BCl2N3O5 Molecular Weight: 462.18 PubChem CID: 137331954 Isomeric SMILES: B1([C@H](CC2=C(O1)C(=CC=C2)C(=O)O)NC(=O)CC3CCC(CC3)NCCN)O.Cl.Cl