标签归档：dorzolamide

Dorzolamide-d5

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Dorzolamide-d5 

Dorzolamide-d5 (L671152-d5) 是 Dorzolamide 的氘代物。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-d5

Dorzolamide-d5 Chemical Structure

CAS No. : 1227097-70-2

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生物活性

Dorzolamide-d5 (L671152-d5) is the deuterium labeled Dorzolamide. 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][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

329.47

Formula

C10H11D5N2O4S3
CAS 号

1227097-70-2
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. 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.

    [3]. 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.

    [4]. 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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Dorzolamide(Synonyms: 多佐胺; L671152; MK507)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务