[CAS NO. 452-35-7] Ethoxzolamide
PRODUCTS SPECIFICATIONS [452-35-7]
DESCRIPTION [452-35-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 258.32 |
| Molecular Formula | C9H10N2O3S2 |
| SMILES | O=S(C1=NC2=CC=C(OCC)C=C2S1)(N)=O |
Summary
Ethoxzolamide is a carbonic anhydrase inhibitor with K i of 1 nM.
IC50 & Target
Ki: 1 nM (carbonic anhydrase) [1]
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 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 [1] . 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 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 387.12 mM )
H 2 O : 1 mg/mL ( 3.87 mM ; ultrasonic and warming and heat to 80°C)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.8712 mL | 19.3558 mL | 38.7117 mL |
| 5 mM | 0.7742 mL | 3.8712 mL | 7.7423 mL |
| 10 mM | 0.3871 mL | 1.9356 mL | 3.8712 mL |
References
- [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.
- [3] Song Gao, et al. Development and validation of an UPLC-MS/MS method for the quantification of ethoxzolamide in plasma and bioequivalent buffers: Applications to absorption, brain distribution, and pharmacokinetic studies. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Apr 1; 0: 54–59.
Synonyms