| Identification | Back Directory | [Name]
VNRX-5133 hydrochloride | [CAS]
2244235-49-0 | [Synonyms]
VNRX-5133 hydrochloride
Taniborbactam hydrochloride
Taniborbactam dihydrochloride | [Molecular Formula]
C19H29BClN3O5 | [MDL Number]
MFCD32708520 | [MOL File]
2244235-49-0.mol | [Molecular Weight]
425.72 |
| Hazard Information | Back Directory | [Uses]
Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam hydrochloride has IC50s 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[1][2]. | [in vivo]
A single dose of Cefepime (HY-B0692) (32 mg/kg)/Taniborbactam hydrochloride (VNRX-5133 hydrochloride; 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 hydrochloride (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 hydrochloride has a T1/2 of 0.16 hours, a CL of 618 mL/h/kg, and a Vss of 143 mL/kg for mice[2].
| [References]
[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. DOI:10.1021/acs.jmedchem.9b00911
[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. DOI:10.1021/acs.jmedchem.9b01518 |
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cjbscvictory
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13348960310 |
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https://www.weikeqi-biotech.com/ |
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