Dorzolamide(Synonyms: 多佐胺; L671152; MK507)

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Dorzolamide (Synonyms: 多佐胺; L671152; MK507)

Dorzolamide (L671152) 是有效的碳酸酐酶 carbonic anhydrase II 的抑制剂，其对红细胞 CA-II 和 CA-I 的 IC50 值分别为 0.18 nM 和 600 nM。

Dorzolamide(Synonyms: 多佐胺; L671152; MK507)

Dorzolamide Chemical Structure

CAS No. : 120279-96-1

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Dorzolamide 的其他形式现货产品:

Dorzolamide hydrochloride

生物活性

Dorzolamide (L671152) 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].

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Swiss albino mice (EAC solid tumor)[3].
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.

Clinical Trial

分子量

324.44

Formula

C10H16N2O4S3
CAS 号

120279-96-1
中文名称

多佐胺
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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