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硝苯地平 /Nifedipine {[allProObj[0].p_purity_real_show]}

货号:A134096 同义名: BAY-a-1040;BAY 1040

Nifedipine 是一种钙通道阻滞剂,对 L-型钙通道具有高亲和力,IC50 值为 10 nM。Nifedipine 具有抗高血压和抗心绞痛作用,可用于心血管疾病的研究。

Nifedipine 化学结构 CAS号:21829-25-4
Nifedipine 化学结构
CAS号:21829-25-4
Nifedipine 3D分子结构
CAS号:21829-25-4
Nifedipine 化学结构 CAS号:21829-25-4
Nifedipine 3D分子结构 CAS号:21829-25-4
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Nifedipine 纯度/质量文件 产品仅供科研

货号:A134096 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Ca2+ channel-like protein Calcium Channel Cav 2.2 其他靶点 纯度
CDC25B-IN-2 Akt 99%+
Clevidipine 97%
Verapamil HCl 99%
Amlodipine 99%
Amlodipine maleate 98%
(+)-cis-Diltiazem HCl 95%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

99%+
Tanshinone IIA sulfonate sodium 98%
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

99%+
Dronedarone Hydrochloride 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

98%
Efonidipine HCl monoethanolate 98%
Cinnarizine 98%
SEA0400 ++

NCX, IC50: 33 nM

ERK,p38 MAPK,ROS 99%+
Fasudil HCl Rho,PKA 98%
ML-9 MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

95%
Lomerizine 2HCl 98%
Efonidipine 98%
Levamlodipine 97%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

97%
Isradipine 98%
Lacidipine 98%
Lercanidipine 98%
Loureirin B Potassium Channel 99%+
Tetracaine HCl 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

98%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

98%
Nicardipine 98%
Wilforgine 98+%
Econazole 99%+
Ginsenoside Rd NF-κB 98%
Fendiline HCl 98+%
Mesaconitine 98%
Tetrandrine 95%
Nifedipine 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

95+%
Azelnidipine 97%
Levetiracetam 98%
Nimodipine 95%
Benidipine HCl 98%
Pinaverium bromide 98%
Pranidipine 98%
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

97%
Cilnidipine 98%
Cinepazide Maleate 98%
Terfenadine 98%
YM-58483 99%+
Ranolazine 98%
Praeruptorin A p38 MAPK,Akt 98%
Ranolazine 2HCl 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

98%
Levamlodipine besylate 97%
Carboxyamidotriazole Orotate 98%
IGS-1.76 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

++++

Cav 2.2, IC50: 0.001 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Nifedipine 生物活性

靶点
  • Calcium Channel

描述 L-type calcium (Ca2+) channel mediates influx of calcium ions into the cytoplasm, and thereby triggers calcium release from the sarcoplasm. Calcium channel also plays an important role in excitation-contraction coupling in the heart and is required for normal heart development and normal regulation of heart rhythm. Nifedipine is a L-type calcium channel antagonist. In a [3H]-thymidine incorporation assay for rat vascular smooth muscle cells growth evaluation, treatment of nifedipine dose-dependently decreased the values of [3H]-thymidine incorporation to 63.82 ± 4.31%, 22.68 ± 1.22% and 5.45 ± 3.26% of those of the control, respectively, at the concentrations of 1 μM, 10 μM and 100 μM[3]. In an electrophysiology assay reported, the sustained inward current activated by 10 mM caffeine at -80 mV was completely inhibited by 1 μM nifedipine. In the absence of caffeine, nifedipine had no effect on the resting current[4]. In a balloon catheterization experiment in rats, nifedipine was administrated at a low dose of 0.3 mg/kg daily or at a high dose of 3 mg/kg daily. Treatment with nifedipine resulted in a distinct change in the size of intimal thickening in a dose-dependent fashion compared to that of the control[3]. According to another report, nifedipine also has anti-ulcer effects. In a HCI plus ethanol induced gastric mucosal injury model in rats, a single oral dose of nifedipine at the doses of 20 mg/kg or 40 mg/kg prevented the gastric mucosal injury[5]. In an acetic acid induced gastric ulcer model, nifedipine was given twice daily orally at the doses of 10 mg/kg, 20 mg/kg or 40 mg/kg for 14 consecutive days. The treatments of nifedipine dose dependently promoted the ulcer healing[5].

Nifedipine 动物研究

Dose Mice: 30 mg/kg[3] (i.p.), 40 mg/kg[4] (i.p.)
Administration i.p.

Nifedipine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00000102 Congenital Adrenal Hyperplasia Phase 1 Phase 2 Completed - United States, South Carolina ... 展开 >> Medical University of South Carolina Charleston, South Carolina, United States 收起 <<
NCT01010048 Urinary Calculus Phase 4 Unknown December 2010 China, Chongqing ... 展开 >> The First Affiliated Hospital, ChongQing medical University Recruiting ChongQing, Chongqing, China, 400016 Contact: Yunfeng He, Doctor    86-23-89011121       Contact: Xiaohou Wu, Doctor    86-23-89011122 收起 <<
NCT00280462 Ocular Physiology ... 展开 >> Regional Blood Flow 收起 << Not Applicable Completed - Austria ... 展开 >> Department of Clinical Pharmacology Vienna, Austria, 1090 收起 <<

Nifedipine 参考文献

[1]Ding Y, Vaziri ND. Nifedipine and diltiazem but not verapamil up-regulate endothelial nitric-oxide synthase expression. J Pharmacol Exp Ther. 2000 Feb;292(2):606-9.

[2]Zhang X, Anderson JW, et al. Characterization of nifedipine block of the human heart delayed rectifier, hKv1.5. J Pharmacol Exp Ther. 1997 Jun;281(3):1247-56.

[3]Hirata A, Igarashi M, Yamaguchi H, Suwabe A, Daimon M, Kato T, Tominaga M. Nifedipine suppresses neointimal thickening by its inhibitory effect on vascular smooth muscle cell growth via a MEK-ERK pathway coupling with Pyk2. Br J Pharmacol. 2000 Dec;131(8):1521-30. doi: 10.1038/sj.bjp.0703730. PMID: 11139427; PMCID: PMC1572490.

[4]Curtis TM, Scholfield CN. Nifedipine blocks Ca2+ store refilling through a pathway not involving L-type Ca2+ channels in rabbit arteriolar smooth muscle. J Physiol. 2001 May 1;532(Pt 3):609-23. doi: 10.1111/j.1469-7793.2001.0609e.x. PMID: 11313433; PMCID: PMC2278590.

[5]Suzuki Y, Ishihara M, Segami T, Ito M. Anti-ulcer effects of antioxidants, quercetin, alpha-tocopherol, nifedipine and tetracycline in rats. Jpn J Pharmacol. 1998 Dec;78(4):435-41. doi: 10.1254/jjp.78.435. PMID: 9920200.

Nifedipine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.89mL

0.58mL

0.29mL

14.44mL

2.89mL

1.44mL

28.87mL

5.77mL

2.89mL

Nifedipine 技术信息

CAS号21829-25-4
分子式C17H18N2O6
分子量 346.335
别名 BAY-a-1040;BAY 1040
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 105 mg/mL(303.18 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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