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Tioxolone is a metalloenzyme carbonic anhydrase I inhibitor with a Ki of 91 nM. Tioxolone lacks sulfonamide, sulfamate, or hydroxamate functional groups that are typically found in therapeutic carbonic anhydrase (CA) inhibitors, such as acetazolamide. Tioxolone is proposed to be a prodrug inhibitor that is cleaved via a CA II zinc-hydroxide mechanism known to catalyze the hydrolysis of esters. When tioxolone binds in the active site of CA II, it is cleaved and forms 4-mercaptobenzene-1,3-diol via the intermediate S- (2,4-thiophenyl) hydrogen thiocarbonate. The esterase cleavage product binds to the zinc active site via the thiol group and is therefore the active CA inhibitor, while the intermediate is located at the rim of the active-site cavity.
| Molecular Weight | 168.17 |
| Formula | C7H4O3S |
| CAS Number | 4991-65-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Carbonic Anhydrase Products |
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| Benzthiazide
Benzthiazide is a thiazide diuretic, promoting water loss from the body. |
| Brinzolamide
Brinzolamide (Brinzolamide) is a potent and effective carbonic anhydrase-II inhibitor with an IC50 of 3.19 nM.In addition, Brinzolamide reduces intraocular aqueous humor production in the eye and may be used in studies related to glaucoma. |
| Ethoxzolamide
Ethoxzolamide is an inhibitor of the metalloenzyme carbonic anhydrase, which inhibits hCA I, hCA II, hCA IV, hCA VI and hCA VII with Ki of 25 nM, 8 nM, 93 nM, 43 nM and 0.8 nM, respectively. |
| Fluorometholone Acetate
Fluorometholone Acetate is a synthetic corticosteroid and a potent carbonic anhydrase (CA) inhibitor with IC50s of 2.18 μM for hCA-I and 17.5 μM for hCA-II. It has anti-inflammatory activity and may be used in studies related to steroid-responsive ocular inflammation. |
| Methazolamide
Methazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively. |
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