CAS NO: | 1613268-23-7 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
Molecular Weight (MW) | 389.26 |
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Formula | C19H28BN3O5 |
CAS No. | 1613268-23-7 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility(In vitro) | DMSO: 10 mM |
Water: N/A | |
Ethanol: N/A | |
Chemical Name | 3-(2-((1r,4r)-4-((2-aminoethyl)amino)cyclohexyl)acetamido)-2-hydroxy-3,4-dihydro-2H-benzo[e][1,2] oxaborinine-8-carboxylic acid |
Synonyms | VNRX-5133; VNRX5133; VNRX 5133 |
In Vitro | In vitroactivity: Taniborbactam hydrochloride (VNRX-5133 hydrochloride) 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 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. |
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In Vivo | A single dose of cefepime (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. |
Animal model | Mouse |
Formulation & Dosage | 32 mg/kg |
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.
[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. |