(S)-Nicardipine
(Synonyms: (S)-YC-93 free base) 目录号 : GC68476(S)-Nicardipine ((S)-YC-93 free base) 是 Nicardipine 的低活性的 S 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 可用于研究慢性心绞痛以及控制血压。
Cas No.:76093-36-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(S)-Nicardipine ((S)-YC-93 free base) is the less active S enantiomer of Nicardipine. Nicardipine 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. | 76093-36-2 | SDF | Download SDF |
| 别名 | (S)-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。 | ||
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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 |
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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。
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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.
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors
J Med Chem 1996 Jul 19;39(15):2980-9.PMID:8709132DOI:10.1021/jm9600205.
1,4-Dihydropyridine and pyridine derivatives bound to three subtypes of adenosine receptors in the micromolar range. Affinity was determined in radioligand binding assays at rat brain A1 and A2A receptors using [3H]-(R)-PIA [[3H]-(R)-N6-(phenylisopropyl)adenosine] and [3H]CGS 21680 [[3H]-2-[[4-(2-carboxyethyl)phenyl]ethylamino]-5'-(N-ethylcarbamoyl++ +) adenosine], respectively. Affinity was determined at cloned human and rat A3 receptors using [125I]AB-MECA [N6-(4-amino-3-iodobenzyl)-5'-(N-methylcarbamoyl)adenosine]. Structure-activity analysis at adenosine receptors indicated that sterically bulky groups at the 4-, 5-, and 6-positions are tolerated. (R,S)-Nicardipine, 12, displayed Ki values of 19.6 and 63.8 microM at rat A1 and A2A receptors, respectively, and 3.25 microM at human A3 receptors. Similarly, (R)-niguldipine, 14, displayed Ki values of 41.3 and 1.90 microM at A1 and A3 receptors, respectively, and was inactive at A2A receptors. A preference for the R- vs the S-enantiomer was observed for several dihydropyridines at adenosine receptors, in contrast with the selectivity at L-type Ca2+ channels. A 4-trans-beta-styryl derivative, 24, with a Ki value of 0.670 microM at A3 receptors, was 24-fold selective vs A1 receptors (Ki = 16.1 microM) and 74-fold vs A2A receptors (Ki = 49.3 microM). The affinity of 24 at L-type Ca2+ channels, measured in rat brain membranes using [3H]isradipine, indicated a Ki value of 0.694 microM, and the compound is thus nonselective between A3 receptors and L-type Ca2+ channels. Inclusion of a 6-phenyl group enhanced A3 receptor selectivity: Compound 28 (MRS1097; 3,5-diethyl 2-methyl-6-phenyl-4-(trans-2-phenylvinyl)-1,4(R,S)-dihydro-pyridin e-3, 5-dicarboxylate) was 55-fold selective vs A1 receptors, 44-fold selective vs A2A receptors, and over 1000-fold selective vs L-type Ca2+ channels. In addition, compound 28 attenuated the A3 agonist-elicited inhibitory effect on adenylyl cyclase. Furthermore, whereas nicardipine, 12, displaced radioligand from the Na(+)-independent adenosine transporter with an apparent affinity of 5.36 +/- 1.51 microM, compound 28 displaced less than 10% of total binding at a concentration of 100 microM. Pyridine derivatives, when bearing a 4-alkyl but not a 4-phenyl group, maintained affinity for adenosine receptors. These findings indicate that the dihydropyridines may provide leads for the development of novel, selective A3 adenosine antagonists.
Effect of UK-84149 on voltage-activated calcium currents of single smooth muscle cells from guinea-pig and rabbit jejunum and rabbit coronary artery
Br J Pharmacol 1995 Apr;114(8):1657-65.PMID:7599936DOI:10.1111/j.1476-5381.1995.tb14954.x.
1. Smooth muscle cells of the longitudinal muscle of the guinea-pig and the rabbit jejunum and rabbit coronary artery were dispersed by enzyme treatment and recordings of membrane current were made in the standard whole cell voltage-clamp mode and by perforated patch technique. The effect of UK-84149 on the voltage-dependent calcium inward current of single isolated smooth muscle was studied at room temperature. 2. When inward and outward currents were evoked by stepping to 0 mV or + 10 mV from -80 mV every 20 S, UK-84149 reduced the voltage-dependent inward current in guinea-pig jejunum smooth muscle cells with a ID50 of 2.3 microM, and also reduced voltage-dependent outward current with a ID50 of 7.2 microM. The effect of UK-84149 was difficult to wash out. 3. The inactivation of the inward current was studied by holding at various potentials for 10 S before evoking inward current at a test potential of 0 mV. The voltage-inactivation curve was shifted to the left by 3 microM UK-84149. The voltage at which current was 50% available (Vh) was changed from -37 +/- 2 mV to -50 mV +/- 2.2 (n = 6, means +/- S.e. mean). 4. When inward current was evoked by stepping to 0 mV from -80 mV for 50 ms, every 20 S, nicardipine immediately, and verapamil and UK-84149 slowly, reduced the peak amplitude. Inhibition by the latter two drugs depended on the number of stimulations applied. So, like verapamil, UK-84149 had a use-dependent action. 5. The effect of UK-84149 on inward current from rabbit jejunum and coronary artery smooth muscle cells was compared with the effect of nicardipine and D600. When inward current was evoked by stepping to 0 mV from - 80 mV every 20 S, UK-84149 inhibited inward currents from both types of smooth cell with an ID50 of 1.7 microM for jejunum and an ID50 of 3.2 microM for coronary artery. ID50 values of D600 were 8.1 microM for jejunum and 3.9 microM for coronary artery. ID50 values of nicardipine were 24 nM for jejunum and 12 nM for coronary artery.6. The results of the present studies indicate that UK-84149 has a calcium-antagonist action that can explain its inhibitory action on bowel motility. Its bowel selectivity may arise due to its use-dependent,and persistent, action.