尼群地平 /Nitrendipine
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货号：A122241
同义名：
BAY-E-5009;Bayotensin
Nitrendipine is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
Nitrendipine 化学结构
Nitrendipine 3D分子结构
规格
价格
会员价
库存
数量
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Nitrendipine 纯度/质量文件 产品仅供科研
货号：A122241
标准纯度：
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Nitrendipine 质控信息
自噬 亚型比较
Calcium Channel 亚型比较
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
++
ROS,p38 MAPK,ERK
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
++++
[3 H]nitrendipine, Ki: 0.21 nM
95+%
Azelnidipine
✔
97%
Levetiracetam
✔
98%
Nimodipine
✔
95%
Benidipine HCl
✔
98%
Pinaverium bromide
✔
98%
Pranidipine
✔
98%
NP118809
+
N-type Ca2+ channel, IC50: 0.11 μM
L-type calcium channel, IC50: 12.2 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
++++
++++
99%+
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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
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] 3 H 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] [4] [5] [6]
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
-
-
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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.
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Nitrendipine 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
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
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