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 In Vitro Taniborbactam 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. ? 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:β-lactamase
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Taniborbactam hydrochloride
CAS number：2244235-49-0 molecular formula：C19H30BCl2N3O5
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| Chinese alias | 盐酸坦尼博巴坦 | ||
| English alias | Taniborbactam HCl | AKOS040739828 | Taniborbactam hydrochloride | Taniborbactam hydrochloride [USAN] | Vnrx5133 dihydrochloride | VNRX-5133 (hydrochloride) | (R)-3-(2-((1S,4R)-rel-4-((2-Aminoethyl)amino)cyclohexyl)acetamido)-2-hydroxy-3,4-dihydro-2H-benzo | ||
| CAS number | 2244235-49-0 | molecular formula | C19H30BCl2N3O5 |
| molecular weight | 462.18 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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