Bioactivity | 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]. |
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]。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. 0 --> Nicardipine-d4 hydrochloride 相关抗体: |
In Vivo | 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. |
Formula | C26H26D4ClN3O6 |
Molar Mass | 520.01 |
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]. Charnet P, et al. Electrophysiological analysis of the action of nifedipine and nicardipine on myocardial fibers. Fundam Clin Pharmacol. 1987;1(6):413-31. [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. |