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.
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- CAS No.: 2209871-83-8
- 화학식: C13H18FN3O5
- 분자량:315.30
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Beta-lactamase Isoforms
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Biological Activity
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2209871-83-8
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분자량 315.30
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화학식 C13H18FN3O5
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)