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1842399-68-1

1842399-68-1 structure
1842399-68-1 structure
  • Name: Ledaborbactam etzadroxil
  • Chemical Name: [(2-Ethylbutanoyl)oxy]methyl (3R)-2-hydroxy-3-(propionylamino)-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylate
  • CAS Number: 1842399-68-1
  • Molecular Formula: C19H26BNO7
  • Molecular Weight: 391.22
  • Catalog: Signaling Pathways Anti-infection Bacterial
  • Create Date: 2022-01-12 07:39:58
  • Modify Date: 2024-01-16 20:23:00
  • Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor[1].

Name [(2-Ethylbutanoyl)oxy]methyl (3R)-2-hydroxy-3-(propionylamino)-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylate
Synonyms 2H-1,2-Benzoxaborin-8-carboxylic acid, 3,4-dihydro-2-hydroxy-3-[(1-oxopropyl)amino]-, (2-ethyl-1-oxobutoxy)methyl ester, (3R)-
[(2-Ethylbutanoyl)oxy]methyl (3R)-2-hydroxy-3-(propionylamino)-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylate
Description Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor[1].
Related Catalog
Target

β-Lactamase[1]

In Vivo Upon dosing the Ledaborbactam etzadroxil (VNRX-7145) in mice, dogs, and monkeys, Ledaborbactam etzadroxil (5-10 mg/kg) demonstrates the most consistent oral bioavailability across species (F = 61-82%)[1]. In intestinal S9, Ledaborbactam etzadroxil is rapidly cleaved with short half-lives in all species with the exception of beagle dogs. The half-life in human plasma is short at about 11 min, which is closer to what was observed in the rodent species compared to the longer half-lives in dogs (43.9 min) and monkeys (22.0 min)[1]. In vivo efficacy is demonstrated in a lethal murine septicemia model by dosing Ledaborbactam etzadroxil (orally) with Ceftibuten. The ED50 value of 12.9 mg/kg[1].
References

[1]. Robert E Trout, et al. Discovery of VNRX-7145 (VNRX-5236 Etzadroxil): An Orally Bioavailable β-Lactamase Inhibitor for Enterobacterales Expressing Ambler Class A, C, and D Enzymes. J Med Chem. 2021 Jul 22;64(14):10155-10166.

Density 1.2±0.1 g/cm3
Molecular Formula C19H26BNO7
Molecular Weight 391.22
Exact Mass 391.180237
Index of Refraction 1.531