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Nilvadipine {[allProObj[0].p_purity_real_show]}

货号:A382623 同义名: FR34235;FK235

Nilvadipine is a potent calcium channel blocker with an IC50 of 0.03 nM.

Nilvadipine 化学结构 CAS号:75530-68-6
Nilvadipine 化学结构
CAS号:75530-68-6
Nilvadipine 3D分子结构
CAS号:75530-68-6
Nilvadipine 化学结构 CAS号:75530-68-6
Nilvadipine 3D分子结构 CAS号:75530-68-6
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Nilvadipine 纯度/质量文件 产品仅供科研

货号:A382623 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

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 ++++

[3H]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 ++++

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。

Nilvadipine 生物活性

靶点
  • Calcium Channel

    Calcium channel, IC50:0.03 nM

描述 Nilvadipine is a potent calcium channel antagonist, and the IC50 value is around 0.1 nM. Nilvadipine, acting as an inhibitor of spleen tyrosine kinase (SYK), is effective at reducing inflammation, tau hyperphosphorylation and amyloid production in AD mouse models[3]. Nilvadipine (FR34235) was also calcium antagonist with IC50 of 3.3 X 10(-11) M. FR34235 should be useful for preventing and treating atherosclerosis[4]. Nicardipine, which showed an antioxidant effect only before exposure to active oxygen and reduced the DHF (dihydroxyfumarate) auto-oxidation rate, was mainly a preventive antioxidant[5]. Nilvadipine (3.2 mg/kg, i.p.) significantly prevented the impairment of spatial memory and neuronal apoptosis in this model[6]. Treatment with Nilvadipine mitigated the TBI-induced inflammatory response in aged r-mTBI (Mild traumatic brain injury) animals and significantly improved spatial memory[7].

Nilvadipine 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
NCT02017340 Alzheimer's Disease Phase 3 Completed - France ... 展开 >> Centre Hospitalier Universitaire d'Amiens (CHU Amiens) Amiens, France Centre Hospitalier Universitaire de Bethune (CH Bethune) Bethune, France Centre Hospitalier Universitaire de Caen (CHU Caen) Caen, France Centre Hospitalier Universitaire de Calais (CHU Calais) Calais, France Centre Hospitalier Universitaire de Lens (CHU Lens) Lens, France Centre Hospitalier Regional et Universitaire de Lille (CHRU Lille) Lille, France Centre Hospitalier Universitaire de Saint Philibert (GHICL) Lille, France Germany University of Ulm Ulm, Germany Greece "G. Papanicolaou" Hospital Athens, Greece "G.Papageorgiou" Hospital Athens, Greece AXEPA Hospital Athens, Greece Hungary Szeged University Szeged, Hungary Ireland University College Cork Cork, Ireland St James Hospital Dublin, Ireland Italy Hospital of Brescia Brescia, Italy Hospital Castellanza Castellanza, Italy Hospital of Genoa Genoa, Italy Hospital of Milan Milan, Italy Netherlands Hospital of Arnhem Arnhem, Netherlands Hospital of Maastricht Maastricht, Netherlands Hospital of Nijmegen Nijmegen, Netherlands Sweden Gothenburg Univeristy Gothenburg, Sweden United Kingdom Kings College London London, United Kingdom 收起 <<

Nilvadipine 参考文献

[1]Ozawa Y, Hayashi K, et al. Renal afferent and efferent arteriolar dilation by nilvadipine: studies in the isolated perfused hydronephrotic kidney. J Cardiovasc Pharmacol. 1999 Feb;33(2):243-7.

[2]Nomoto A, Mutoh S, et al. Smooth muscle cell migration induced by inflammatory cell products and its inhibition by a potent calcium antagonist, nilvadipine. Atherosclerosis. 1988 Aug;72(2-3):213-9.

[3]Morin A, Mouzon B, Ferguson S, Paris D, Browning M, Stewart W, Mullan M, Crawford F. Nilvadipine suppresses inflammation via inhibition of P-SYK and restores spatial memory deficits in a mouse model of repetitive mild TBI. Acta Neuropathol Commun. 2020 Oct 19;8(1):166

[4]Nomoto A, Hirosumi J, Sekiguchi C, Mutoh S, Yamaguchi I, Aoki H. Antiatherogenic activity of FR34235 (Nilvadipine), a new potent calcium antagonist. Effect on cuff-induced intimal thickening of rabbit carotid artery. Atherosclerosis. 1987 Apr;64(2-3):255-61

[5]Sugawara H, Tobise K, Kikuchi K. Antioxidant effects of calcium antagonists on rat myocardial membrane lipid peroxidation. Hypertens Res. 1996 Dec;19(4):223-8

[6]Iwasaki K, Egashira N, Takagaki Y, Yoshimitsu Y, Hatip-Al-Khatib I, Mishima K, Fujiwara M. Nilvadipine prevents the impairment of spatial memory induced by cerebral ischemia combined with beta-amyloid in rats. Biol Pharm Bull. 2007 Apr;30(4):698-701

[7]Morin A, Mouzon B, Ferguson S, Paris D, Saltiel N, Lungmus C, Mullan M, Crawford F. Treatment With Nilvadipine Mitigates Inflammatory Pathology and Improves Spatial Memory in Aged hTau Mice After Repetitive Mild TBI. Front Aging Neurosci. 2018 Oct 11;10:292

Nilvadipine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.97mL

2.59mL

1.30mL

25.95mL

5.19mL

2.59mL

Nilvadipine 技术信息

CAS号75530-68-6
分子式C19H19N3O6
分子量 385.371
别名 FR34235;FK235;Nilvadipine, Escor, Nivadil, FR-34235, FK-235;SKF 102362;(±)-Nilvadipine;CL 287,389
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,Sealed in dry,2-8°C

溶解度

DMSO: 50 mg/mL(129.75 mM),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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