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/ Nifedipine/硝苯地平

Nifedipine/硝苯地平 {[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/硝苯地平 化学结构 CAS号：21829-25-4
Nifedipine/硝苯地平 化学结构
CAS号：21829-25-4
Nifedipine/硝苯地平 3D分子结构
CAS号：21829-25-4
Nifedipine/硝苯地平 化学结构 CAS号：21829-25-4
Nifedipine/硝苯地平 3D分子结构 CAS号：21829-25-4
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Nifedipine/硝苯地平 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]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
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 ✔ 99%
Zegocractin ++

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

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

hCaV3.2, IC50: 110 nM

hCaV3.1, IC50: 50 nM

 		99%+
Dronedarone HCl ✔ 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

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

NCX, IC50: 33 nM

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

Calcium channel, Ki: 68 nM

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

L-type Cav1.2, IC50: 10 nM

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

Calcium channel, IC50: 2.6 nM

 		99%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

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

Calcium channel, IC50: 0.03 nM

 		95%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

 		95+%
Azelnidipine ✔ 97%
Levetiracetam ✔ 98%
Nimodipine ✔ 95%
Benidipine HCl ✔ 98%
Pinaverium bromide ✔ 98%
Pranidipine ✔ 99%
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

 		95%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

 		97%
Cilnidipine ✔ 99%
Cinepazide Maleate ✔ 99% (HPLC)
Terfenadine ✔ 98%
YM-58483 ✔ 99%+
Amiloride HCl ✔ 98%
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/硝苯地平 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/硝苯地平 细胞实验

Cell Line
Concentration Treated Time Description References
Rat aortic smooth muscle cells 25 and 100 nM 30 min To investigate the effect of Nifedipine on Ang II-induced NADPH oxidase activity, results showed that Nifedipine significantly attenuated Ang II-induced NADPH oxidase activity. J Mol Cell Cardiol. 2015 Oct;87:152-9.
Mouse liver S9 fraction 50 μM 40 min To test the activity of mouse hepatic CYP3A11, the results showed that the generation of oxidized nifedipine in control mice was significantly higher than in treated mice Acta Pharm Sin B. 2021 Dec;11(12):3820-3835.
Gastric Smooth Muscle Cells 10 μM Used to test the occurrence of L-type calcium current (ICa,L). Int J Mol Sci. 2020 Dec 17;21(24):9617.
CAFs 2.5 μM 24 h To assess the effect of Nifedipine on the activated state of CAFs, results showed that Nifedipine reduced CAF motility and ECM remodeling ability, and decreased MMP-2 release. J Exp Clin Cancer Res. 2024 Jun 11;43(1):161.
DU145 cells 2.5 μM 24 h To evaluate the effect of Nifedipine-treated CAFs on the growth of DU145 cells, results showed that Nifedipine significantly inhibited the growth of DU145 cells. J Exp Clin Cancer Res. 2024 Jun 11;43(1):161.
LNCaP cells 14.69 µM 72 h Nifedipine showed dose-dependent antiproliferative effects in LNCaP cells with an IC50 value of 14.69 µM. Cancer Biol Med. 2021 Apr 24;19(1):74–89.
DU145 cells 26.66 µM 72 h Nifedipine showed dose-dependent antiproliferative effects in DU145 cells with an IC50 value of 26.66 µM. Cancer Biol Med. 2021 Apr 24;19(1):74–89.
MGC-803 cells 20.73 µM 72 h Nifedipine showed toxicity in the MGC-803 cell line with an IC50 value of 20.73 µM. Cancer Biol Med. 2021 Apr 24;19(1):74–89.
hSSC-derived cells 5 μM 3 weeks To determine the Ca2+ influx in hSSC-derived cells, results showed that nifedipine significantly reduced the Ca2+ influx. Stem Cell Res Ther. 2019 Jun 27;10(1):195.

Nifedipine/硝苯地平 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Cacna1d KO mice Apical administration 10 μM Single dose To investigate the effect of Nifedipine on ileal calcium absorption in Cacna1d KO mice, results showed that Nifedipine significantly inhibited ileal calcium absorption in WT mice but not in Cacna1d KO mice. Cell Mol Gastroenterol Hepatol. 2019;8(4):625-642
Mice Awake and freely moving mouse model Intraperitoneal injection 1 mg/kg Single administration, observed for 6 hours To investigate the modulation of JWH-018-induced cardiovascular and respiratory responses by Nifedipine. Results showed that Nifedipine did not significantly reverse the JWH-018-induced bradycardia but slightly reduced the JWH-018-induced tachyarrhythmic events during the last two hours of the experiment. Additionally, Nifedipine restored the JWH-018-induced reduction in breath rate and SpO2 immediately after administration. Int J Mol Sci. 2023 Apr 19;24(8):7515
Hph-1 mice Ang II-induced abdominal aortic aneurysm model Oral 5 and 20 mg/kg Once daily for 2 weeks To investigate the effect of Nifedipine on AAA formation, results showed that Nifedipine significantly reduced the incidence of AAA and improved eNOS coupling and NO bioavailability. J Mol Cell Cardiol. 2015 Oct;87:152-9.
Mice Chronic colitis model Oral 20 mg/kg Once daily for 14 weeks To study the effects of long-term exposure to RTS and/or DSS on the liver and intestines of mice, the results showed that RTS exposure caused intestinal injury, and DSS exacerbated RTS-induced liver injury Acta Pharm Sin B. 2021 Dec;11(12):3820-3835.
SCID mice Prostate cancer xenograft model Intratumoral injection 250 μl 5 consecutive days for 2 weeks To evaluate the effect of Nifedipine-treated CAFs on the growth of prostate cancer xenografts, results showed that Nifedipine significantly inhibited tumor growth. J Exp Clin Cancer Res. 2024 Jun 11;43(1):161.
Male athymic nude mice Prostate cancer xenograft model Intraperitoneal injection 50 mg/kg Once daily for 18 days Nifedipine significantly inhibited the growth of prostate tumors without causing apparent changes. Cancer Biol Med. 2021 Apr 24;19(1):74–89.

Nifedipine/硝苯地平 动物研究

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

Nifedipine/硝苯地平 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/硝苯地平 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/硝苯地平 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/硝苯地平 技术信息

CAS号21829-25-4
分子式C17H18N2O6
分子量 346.33
SMILES Code O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC
MDL No. MFCD00057326
别名 BAY-a-1040; BAY 1040
运输蓝冰
InChI Key HYIMSNHJOBLJNT-UHFFFAOYSA-N
Pubchem ID 4485
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一

Tags: Nifedipine/硝苯地平 |Nifedipine/硝苯地平 | BAY-a-1040 | BAY 1040 | 21829-25-4 | Calcium Channel | 降压 | Nifedipine/硝苯地平 纯度/质量文件 | Nifedipine/硝苯地平 亚型比较 | Nifedipine/硝苯地平 生物活性 | Nifedipine/硝苯地平 动物研究 | Nifedipine/硝苯地平 临床数据 | Nifedipine/硝苯地平 参考文献 | Nifedipine/硝苯地平 实验方案 | Nifedipine/硝苯地平 技术信息

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