| Name | Avibactam free acid |
| Description | Avibactam free acid is a potent β-lactamase inhibitor exhibiting covalent and reversible properties, capable of inhibiting TEM-1, P99, and CTX-M-15 at nanomolar concentrations. Avibactam free acid and Ceftazidime may be combined for treating urinary tract infections. |
| In vitro | Using TEM-1 as the research subject, the inhibitory effect of Avibactam free acid was characterized by measuring the on-rate (acylation) and off-rate (deacylation) of the enzyme. The results showed that the deacylation dissociation rate was 0.045 min⁻¹, providing potential insights into the deacylation pathway of TEM-1 enzyme. Using nuclear magnetic resonance (NMR) and mass spectrometry (MS), we discovered that the deacylation process regenerates intact Avibactam free acid rather than proceeding via hydrolysis [1]. |
| In vivo | In the mouse model infected with Klebsiella pneumoniae strain Y8, Ceftazidime-Avibactam free acid (0.375 mg/g, subcutaneous injection, every 8 hours for 10 days) exhibited significant antibacterial effects and produced certain therapeutic outcomes [3].
In the neutropenic pneumonia mouse model with Pseudomonas aeruginosa infection, following a single subcutaneous injection of Avibactam free acid (64 mg/kg), the mean estimated terminal-phase half-life in mouse plasma was 0.24 hours [3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (12.44 mM), Sonication is recommended.
DMSO : 100 mg/mL (377.02 mM), Sonication is recommended.
|
| Keywords | TEM-1 | CTX-M-15 | Avibactam free acid |
| Inhibitors Related | Neomycin sulfate | Adipic dihydrazide | Levulinic acid | D(+)-Raffinose pentahydrate | Sulfamethoxazole sodium | Terbinafine hydrochloride | Doxycycline | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate | Sodium bicarbonate | BES |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Approved Drug Library | ReFRAME Related Library | Drug Repurposing Compound Library | Anti-Bacterial Compound Library | Bioactive Compounds Library Max |
United States
