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Taniborbactam hydrochloride

Catalog No. T13077 CAS 2244235-49-0

Synonyms: VNRX-5133 hydrochloride

Taniborbactam hydrochloride is a reversible and selective inhibitor of boronic acid-containing pan-spectrum β-lactamase(IC50s of 8-530 nM).

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Taniborbactam hydrochloride, CAS 2244235-49-0

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Taniborbactam hydrochloride is a reversible and selective inhibitor of boronic acid-containing pan-spectrum β-lactamase(IC50s of 8-530 nM).
In vitro	Taniborbactam hydrochloride (VNRX-5133 hydrochloride) (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)[2]. 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(MIC ranges of 16-0.25 and 1-0.125 μg/mL, respectively)[1].
In vivo	In the neutropenic mouse lung infection model, 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 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].

Synonyms	VNRX-5133 hydrochloride
Molecular Weight	462.18
Formula	C19H30BCl2N3O5
CAS No.	2244235-49-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Taniborbactam hydrochloride 2244235-49-0 微生物学 Antibacterial VNRX-5133 hydrochloride Inhibitor inhibitor inhibit

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