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尼群地平 /Nitrendipine 98%

货号：A122241 同义名： BAY-E-5009;Bayotensin Ambeed 开学季，买赠积分，赢豪礼

Nitrendipine is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.

Nitrendipine 化学结构 CAS号：39562-70-4
Nitrendipine 化学结构
CAS号：39562-70-4
Nitrendipine 3D分子结构
CAS号：39562-70-4
Nitrendipine 化学结构 CAS号：39562-70-4
Nitrendipine 3D分子结构 CAS号：39562-70-4
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Nitrendipine 纯度/质量文件 产品仅供科研

货号：A122241 标准纯度： 98%
批次查询： 批次纯度:

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产品名称 Autophagy ↓ 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

 		97%
Hydroxychloroquine sulfate ✔ 99%
Valproic acid sodium ✔ HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

 		99%+
ROC-325 ✔ 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		97%
Lys05 ✔ 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。
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 ++

hCaV3.2, IC50: 110 nM

hCaV3.1, IC50: 50 nM

 		99%+
Dronedarone Hydrochloride ✔ 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

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

NCX, IC50: 33 nM

 		ROS,ERK,p38 MAPK 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。

Nitrendipine 生物活性

靶点

  • Calcium Channel

    Calcium channel, IC50:95 nM
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. Nitrendipine is a L-type calcium channel inhibitor. Based on experiments performed on a whole-cell voltage clamp current recording system, nitrendipine blocked Ca2+ currents potently with half-block by subnanomolar concentrations. The concentration dependence of block had the form expected for 1:1 binding, with an apparent dissociation constant (Kd) of 0.36 nM[3]. In a radioligand binding assay, 3H labeled nitrendipine specifically binded to the microsomal fraction from isolated guinea-pig ileal longitudinal muscle, and the binding pattern was saturable and linear with protein concentration and reversible. The apparent equilibrium dissociation constant was 1.63 ± 0.06 ×10-10 M and the maximum site density was 1.13 ± 0.03 pmol/mg of protein, as determined from scatchard analysis of equilibrium binding at 25ºC[4].

Nitrendipine 动物研究

Dose Rat: 10 mg/kg[3] (i.p.); 1 mg/kg/day[4] (p.o.); 5 mg/kg[5] (i.g.) Mice: 5 mg/kg[6] (p.o.)
Administration i.p., p.o., i.g.

Nitrendipine 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
NCT00892892 Chronic Kidney Disease ... 展开 >> Hypertension 收起 << Phase 4 Withdrawn - Germany ... 展开 >> University of Erlangen-Nuremberg, CRC, med. Clinic 4 Erlangen, Bavaria, Germany, 91054 收起 <<
NCT01074281 - Completed - -
NCT02088450 Isolated Systolic Hypertension Phase 2 Terminated - -

Nitrendipine 参考文献

[1]Peterson BZ, Tanada TN, et al. Molecular determinants of high affinity dihydropyridine binding in L-type calcium channels. J Biol Chem. 1996 Mar 8;271(10):5293-6.

[2]Bean BP. Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state. Proc Natl Acad Sci U S A. 1984 Oct;81(20):6388-92.

[3]Bean BP. Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state. Proc Natl Acad Sci U S A. 1984 Oct;81(20):6388-92. doi: 10.1073/pnas.81.20.6388. PMID: 6093100; PMCID: PMC391929.

[4]Bolger GT, Gengo P, Klockowski R, Luchowski E, Siegel H, Janis RA, Triggle AM, Triggle DJ. Characterization of binding of the Ca++ channel antagonist, [3H]nitrendipine, to guinea-pig ileal smooth muscle. J Pharmacol Exp Ther. 1983 May;225(2):291-309. PMID: 6842393.

Nitrendipine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.87mL

2.77mL

1.39mL

27.75mL

5.55mL

2.77mL

Nitrendipine 技术信息

CAS号39562-70-4
分子式C18H20N2O6
分子量 360.361
别名 BAY-E-5009;Bayotensin;Nitrendipine, Bayotensin, Baypress, Nidrel, Deiten
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 50 mg/mL(138.75 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

IP 2% DMSO+2% Tween80+40% PEG300+water 7 mg/mL clear

PO 0.5% CMC-Na 31 mg/mL suspension

Tags: Nitrendipine | 39562-70-4 | BAY-E-5009 | Calcium Channel | Membrane Transporter/Ion Channel | Neuronal Signaling | Autophagy | Calcium Channel | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Nitrendipine 纯度/质量文件 | Nitrendipine 亚型比较 | Nitrendipine 生物活性 | Nitrendipine 动物研究 | Nitrendipine 临床数据 | Nitrendipine 参考文献 | Nitrendipine 实验方案 | Nitrendipine 技术信息

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