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Nitrendipine

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Chemical Structure| 39562-70-4 同义名 : BAY-E-5009;Bayotensin;Nitrendipine, Bayotensin, Baypress, Nidrel, Deiten
CAS号 : 39562-70-4
货号 : A122241
分子式 : C18H20N2O6
纯度 : 98%
分子量 : 360.361
MDL号 : MFCD00082255
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

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].
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 Phase 4 Withdrawn - Germany ...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 - -
实验方案
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
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.