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.
体外研究
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).
体内研究
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).
Animal Model:
Female Swiss albino mice (EAC solid tumor).
Dosage:
3, 10, or 30 mg/kg/day (synergized mitomycin C).
Administration:
IP, daily for 3 weeks.
Result:
Upregulated TXNIP and p53 while downregulated bcl-2.
Effective in retarding the growth of EAC in mice.
分子式
C10H17ClN2O4S3
分子量
360.90
CAS号
130693-82-2
中文名称
盐酸多佐胺
运输条件
Room temperature in continental US; may vary elsewhere.