(R)-Nicardipine
(Synonyms: (R)-YC-93 free base) 目录号 : GC68475(R)-Nicardipine ((R)-YC-93 free base) 是 Nicardipine 的低活性的 R 型对映异构体。Nicardipine 是一种钙通道 (Calcium Channel) 阻滞剂，可阻断心脏钙通道，IC50 为 1 μM。 Nicardipine 可用于慢性心绞痛以及控制血压的研究。
Cas No.:76093-35-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(R)-Nicardipine ((R)-YC-93 free base) is the less active R enantiomer of Nicardipine. Nicardipine (YC-93) is a Calcium Channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure[1].
[1]. Charnet P, et al. Electrophysiological analysis of the action of nifedipine and nicardipine on myocardial fibers. Fundam Clin Pharmacol. 1987;1(6):413-31.
| Cas No. | 76093-35-1 | SDF | Download SDF |
| 别名 | (R)-YC-93 free base | ||
| 分子式 | C26H29N3O6 | 分子量 | 479.52 |
| 溶解度 | DMSO : 200 mg/mL (417.08 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0854 mL | 10.4271 mL | 20.8542 mL |
| 5 mM | 0.4171 mL | 2.0854 mL | 4.1708 mL |
| 10 mM | 0.2085 mL | 1.0427 mL | 2.0854 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
The difference between nicardipine and its enantiomers on inhibiting vasoconstriction of isolated rabbit thoracic artery
Arch Pharm Res 2005 Mar;28(3):319-24.PMID:15832820DOI:10.1007/BF02977799.
The present study was designed to study the difference effects between nicardipine and its two enantiomers on thoracic artery of rabbit. A high-performance liquid chromatographic method was used to prepare the two enantiomers of nicardipine. The thoracic artery of rabbit was removed. The vessels were cut into 3 mm in width and 15 mm in length spiral strips and immersed into tissue baths. The concentration-response curves of nicardipine and its enantiomers were obtained by cumulative administration of the vasoconstrictors. Nicardipine and the enantiomers could shift the dose-response curves of NE, KCl or CaCl2 to right in a nonparallel manner and decrease the maximum effective in a concentration-depended manner, respectively. The pD2' value of R-(-)-Nicardipine showed significantly effective than that of nicardipine and S-(+)-Nicardipine (P<0.01). There was not obviouse difference between the pD2' value of nicardipine and S-(+)-Nicardipine (P>0.05). The results demonstrate that the stereoselective interaction between R-(-)-Nicardipine and L-calcium channel receptor is more stronger than that of S-(+)-Nicardipine.
[Protection of HOE642 against cardiomyocyte injury caused by anoxia and reoxygenation]
Sichuan Da Xue Xue Bao Yi Xue Ban 2005 Sep;36(5):672-5.PMID:16235534doi
Objective: To investigate the protective effect of calcium antagonists (A/R) injury of cardiomyocytes. Methods: Primary-cultured cardiomyocytes were divided A/R, A/R+nicardipine(Nic), A/R+HOE642, A/R+H7, A/R+PD98059 and control parameters were measured in all groups, intracellular calcium concentration ([Ca2+]i), content, lactate dehydrogenase (LDH) and creative phosphokinase(CK) activity in the activity. The calpain (u-calpain and m-calpain) protein expression levels were measured In comparison with A/R group, A/R + nicardipine (Nic) and A/R + Nic groups showed [Ca2+]i, m-calpain protein expression, LDH and CK content in the medium, a higher activity of PKC and MAPK (P < 0.01). On the contrary, A/R+H7 and A/R+PD98059 LDH and CK content in the medium, and lower ATP content and cell viability as compared 0. 05). Conclusion: The A/R mediated Ca2+ overload resulting from cardiomyocyte injury blocking Ca2+ entry and H+/Na+ exchange, and very likely PKC and MAPK are involved protection against the A/R injury of cardiomyocytes.