Bioactivity | 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]. |
Invitro | 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. 0 --> Dorzolamide-d3 hydrochloride 相关抗体: |
In Vivo | 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. |
Formula | C10H14D3ClN2O4S3 |
Molar Mass | 363.92 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [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. [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. [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. |