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Ethoxzolamide

CAS No. : 452-35-7

MCE 站：Ethoxzolamide

产品活性：Ethoxzolamide 是 carbonic anhydrase 的抑制剂，其 K_i 值为 1 nM。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Carbonic Anhydrase  |  Bacterial

In Vitro: Ethoxzolamide (ETZ) treatment causes >90% inhibition of reporter GFP fluorescence in infected macrophages. Moreover, in a 9-day macrophage survival assay, Ethoxzolamide (ETZ) treatment significantly inhibits the ability of M. tuberculosis to grow intracellularly.

In Vivo: It is discovered that the lipid-soluble ethoxzolamide is converted in vivo to a water-soluble metabolite, while retaining high activity againstt the enzyme. At the minimal dose for maximal effect (4 mg/kg i.v. at 45 min) the IOP lowering is 4.2 mmHg, the concentration in anterior uvea is 2.5 pmol/kg, and the fractional inhibition of the enzyme (i) is 0.9995. The effect declines rapidly, attributable to the very short half-life of drug in plasma, leading to depletion of free drug in the anterior uvea and other tissues. Ethoxzolamide (ETZ) strongly downregulates GFP reporter fluorescence in mouse lungs, with 3-fold inhibition of GFP signal compare to that in the mock-treating control. There is a significant reduction of bacterial survival in the lungs of ETZ-treating mice compare to the mock-treating control.

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