Ethoxzolamide 是 carbonic anhydrase 的抑制剂，其 K_i 值为 1 nM。

Ethoxzolamide is a carbonic anhydrase inhibitor with K i of 1 nM.

Solid

Ki: 1 nM (carbonic anhydrase)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not ind

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Maren TH, et al. Relations among IOP reduction, ocular disposition and pharmacology of the carbonic anhydrase inhibitor ethoxzolamide. Exp Eye Res. 1992 Jul;55(1):73-9.
[2]. Benjamin K. Johnson, et al. The Carbonic Anhydrase Inhibitor Ethoxzolamide Inhibits theMycobacterium tuberculosis PhoPR Regulon and Esx-1 Secretion and Attenuates Virulence. Antimicrob Agents Chemother. 2015 Aug; 59(8): 4436–4445.

In Vitro: DMSO : ≥ 100 mg/mL (387.12 mM)H₂O : 1 mg/mL (3.87 mM; ultrasonic and warming and heat to 80°C)