Bioactivity | Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity[1]. |
Invitro | Component A, caused by an inward flux of CO2 and its subsequent hydration by CA-II, is blocked by Dorzolamide in a dose-dependent manner with an 50% inhibitory concentration IC50 of 2.4 μM (95% confidence interval: 0.5-10.85 μM)[2]. |
In Vivo | Dorzolamide (3, 10, or 30 mg/kg/day, ip) synergized mitomycin C exhibits anti-tumor activity in EAC solid tumor models. Dorzolamide produces a dose-dependent decrease in the calculated ratio (relative value of 57.3±1, 25.5±1.8, and 24.3± 0.7 %, respectively)[3]. Animal Model: |
Name | Dorzolamide hydrochloride |
CAS | 130693-82-2 |
Formula | C10H17ClN2O4S3 |
Molar Mass | 360.90 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. J Biollaz, et al. Whole-blood pharmacokinetics and metabolic effects of the topical carbonic anhydrase inhibitor dorzolamide. Eur J Clin Pharmacol. 1995;47(5):455-60. [2]. Sangly P Srinivas, et al. Inhibition of carbonic anhydrase activity in cultured bovine corneal endothelial cells by dorzolamide. Invest Ophthalmol Vis Sci. 2002 Oct;43(10):3273-8. [3]. Belal M Ali, et al. Dorzolamide synergizes the antitumor activity of mitomycin C against Ehrlich's carcinoma grown in mice: role of thioredoxin-interacting protein. Naunyn Schmiedebergs Arch Pharmacol. 2015 Dec;388(12):1271-82. |