Nicardipine-d₄ hydrochloride  (Synonyms: 盐酸尼卡地平-d₄; YC-93-d₄)

Nicardipine-d₄ hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure^[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]。
Nicardipine (0.1-10 μM；24-48 小时) 降低血管平滑肌细胞 (VSMC) 的活力和增殖，并抑制其迁移能力^[3]。

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

Nicardipine (0.3-10 mg/kg；po) 具有抗高血压特性^[4]。
Nicardipine hydrochloride 的LD₅₀s分别为643 mg/kg (口服) 和557 mg/kg (口服)；18.1 mg/kg (静脉内) 25.0 mg/kg (静脉内)；735 mg/kg (皮下) 和 683 mg/kg (皮下)；雄性和雌性 Sprague-Dawley 大鼠分别为 171 mg/kg (腹膜内) 和 155 mg/kg (腹膜内)^[4]。
Nicardipine hydrochloride 对雄性 Wistar 大鼠的 LD₅₀ 分别为 187 mg/kg (口服) 和 15.5 mg/kg (静脉注射)^[4]。
Nicardipine hydrochloride 的LD₅₀s分别为634 mg/kg (口服) 和650 mg/kg (口服)；20.7 mg/kg (静脉内) 19.9 mg/kg (静脉内)；540 mg/kg (皮下) 和 710 mg/kg (皮下)；雄性和雌性小鼠分别为 144 mg/kg (腹膜内) 和 161 mg/kg (腹膜内)^[4]。

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

520.01

C₂₆H₂₆D₄ClN₃O₆

54527-84-3

盐酸尼卡地平-d₄

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]. Charnet P, et al. Electrophysiological analysis of the action of nifedipine and nicardipine on myocardial fibers. Fundam Clin Pharmacol. 1987;1(6):413-31.  [Content Brief]

  [3]. R Stamatiou, et al. The dihydropyridine calcium antagonist nicardipine reduces aortic smooth muscle cell viability, proliferation and migration. Cardiovascular Research, 2018 Apr,114(1):S43.

  [4]. Sherrin H. Baky. Nic ardipine Hydrochloride.