Dorzolamide-d₃ hydrochloride  (Synonyms: 盐酸多佐胺-d₃; L671152-d₃ hydrochloride; MK507-d₃ hydrochloride)

Dorzolamide-d₃ hydrochloride is deuterated labeled Dorzolamide hydrochloride (HY-B0109A). 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].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
组分 A 由 CO2 的内流及其随后的 CA-II 水合作用引起，被 Dorzolamide hydrochloride 以剂量依赖的方式阻断，IC₅₀ 为 2.4 μM^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Dorzolamide hydrochloride (3、10 或 30 mg/kg/天，腹腔注射) 协同丝裂霉素 C 在 EAC 实体瘤模型中表现出抗肿瘤活性。Dorzolamide hydrochloride 使计算出的比率呈剂量依赖性降低 (相对值分别为 57.3±1、25.5±1.8 和 24.3±0.7%)^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

363.92

C₁₀H₁₄D₃ClN₂O₄S₃

130693-82-2

盐酸多佐胺-d₃

Room temperature in continental US; may vary elsewhere.

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

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. 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.  [Content Brief]

  [4]. 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.  [Content Brief]