ETX0282

ETX0282 is an orally active prodrug, with its active form being ETX1317. ETX0282 and ETX1317 are β-lactamase inhibitors of the dioxolane-dibenzo-p-heptane (DBO) type. ETX0282 exhibits high stability during intestinal absorption and can be efficiently converted into ETX1317 in the liver. ETX0282 alone has no bactericidal activity, but in a mouse model of neutropenic thigh infection, it can significantly reduce bacterial load when used in combination with Cefpodoxime Proxetil (HY-N7101) . ETX0282 can be used for the study of infections caused by drug-resistant Gram-negative bacteria[1][2].

Product Specifications

CAS Number

[2209871-83-8]

UNSPSC

12352005

Target

Beta-lactamase

Related Pathways

Anti-infection

Applications

COVID-19-immunoregulation

Field of Research

Infection

Smiles

O=C(OC(C)C)[C@H](ON1[C@]2([H])C(C)=C[C@@H](C(N)=O)[N@@](C2)C1=O)F

Molecular Formula

C13H18FN3O5

Molecular Weight

315.30

References & Citations

[1]Durand-Réville TF, et al. Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases. J Med Chem. 2020 Nov 12;63 (21) :12511-12525.|[2]O'Donnell J, et al. Pharmacokinetic/Pharmacodynamic Determination and Preclinical Pharmacokinetics of the β-Lactamase Inhibitor ETX1317 and Its Orally Available Prodrug ETX0282. ACS Infect Dis. 2020 Jun 12;6 (6) :1378-1388.