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Taniborbactam dihydrochloride

Catalog No. T13077 CAS 2244235-49-0

Synonyms: VNRX-5133 dihydrochloride, Taniborbactam 2HCl

Taniborbactam dihydrochloride (VNRX-5133 dihydrochloride) is a selective and potent novel cyclic boronic acid β-lactamase inhibitor with antimicrobial activity and significant inhibition of Gram-negative bacteria.Taniborbactam dihydrochloride inhibits KPC Taniborbactam dihydrochloride inhibits KPC-2, AmpC, OXA-48 and VIM-2 and can be used for the study of fungal infections.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Taniborbactam dihydrochloride Chemical Structure

Taniborbactam dihydrochloride, CAS 2244235-49-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 263.00
5 mg	In stock	$ 645.00
10 mg	In stock	$ 987.00
25 mg	10-14 weeks	$ 1,860.00
50 mg	10-14 weeks	$ 2,880.00

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Purity: 97.50%

Purity: 96.43%

ee: 100%

Biological Description

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Description	Taniborbactam dihydrochloride (VNRX-5133 dihydrochloride) is a selective and potent novel cyclic boronic acid β-lactamase inhibitor with antimicrobial activity and significant inhibition of Gram-negative bacteria.Taniborbactam dihydrochloride inhibits KPC Taniborbactam dihydrochloride inhibits KPC-2, AmpC, OXA-48 and VIM-2 and can be used for the study of fungal infections.
Targets&IC50	KPC2:0.5 nM, VIM-2:0.06 nM, VIM-4:0.5 nM, OXA-48:2 nM
In vitro	Taniborbactam dihydrochloride (VNRX-5133 dihydrochloride) exhibits IC50 values of 0.5 nM, 2 nM, 0.5 nM, and 0.06 nM against KPC-2, OXA-48, VIM-4 strains of Klebsiella pneumoniae, and VIM-2 strain of Pseudomonas aeruginosa, respectively[1].The combination of Cefepime/Taniborbactam dihydrochloride (10 μg/mL) and Meropenem/Taniborbactam dihydrochloride shows MIC ranges of 16-0.25 μg/mL and 1-0.125 μg/mL against strains derived from Klebsiella pneumoniae and Escherichia coli, respectively[2].
In vivo	In a single-dose mouse lung infection model with neutropenia, a single dose of Cefepime at 32 mg/kg combined with Taniborbactam dihydrochloride (VNRX-5133 dihydrochloride) at 16 mg/kg (subcutaneous injection) results in a reduction of bacterial counts by >4 log10. This combination is effective against K. pneumoniae strains producing CTX-M-14[1].In a combination treatment in a kidney infection model, Cefepime at 16 mg/kg and Taniborbactam dihydrochloride at 16 mg/kg (subcutaneous injection, twice daily for 7 days) lead to a reduction of bacterial counts by >2 log10 in the kidneys, targeting E. coli strains producing CTX-M-15[2].The half-life (T1/2) of Taniborbactam dihydrochloride in mice is 0.16 hours, with a clearance (CL) of 618 mL/h/kg and a volume of distribution at steady state (Vss) of 143 mL/kg[1].

Synonyms	VNRX-5133 dihydrochloride, Taniborbactam 2HCl
Molecular Weight	462.18
Formula	C19H30BCl2N3O5
CAS No.	2244235-49-0

Storage

keep away from direct sunlight,store under nitrogen

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 30 mg/mL (64.91 mM), Sonication is recommended.

DMSO: 100 mg/mL (216.37 mM), Sonication is recommended.

References and Literature

1. 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. 2. Krajnc A, et al. Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases. J Med Chem. 2019 Sep 26;62(18):8544-8556.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

Taniborbactam dihydrochloride 2244235-49-0 Microbiology/Virology Antibacterial Antifungal VNRX 5133 Hydrochloride VNRX5133 Hydrochloride VNRX-5133 dihydrochloride Taniborbactam 2HCl VNRX-5133 Hydrochloride Taniborbactam Hydrochloride inhibitor inhibit

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