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依拉地平 /Isradipine {[allProObj[0].p_purity_real_show]}

货号:A782133 同义名: 伊拉地平 / PN 200-110

Isradipine is a potent L-type calcium channel selective blocker with an IC50 of 34±8 μM.

Isradipine 化学结构 CAS号:75695-93-1
Isradipine 化学结构
CAS号:75695-93-1
Isradipine 3D分子结构
CAS号:75695-93-1
Isradipine 化学结构 CAS号:75695-93-1
Isradipine 3D分子结构 CAS号:75695-93-1
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Isradipine 纯度/质量文件 产品仅供科研

货号:A782133 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,ERK,p38 MAPK 99%+
Fasudil HCl Rho,PKA 98%
ML-9 Akt,MLCK 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 Akt,p38 MAPK 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。

Isradipine 生物活性

靶点
  • Calcium Channel

描述 sradipine is a calcium antagonist with marked vascular selectivity and, in practical terms, is devoid of cardiac effects. Both when used as single drug treatment and in combination with other agents, particularly beta-blockers, isradipine is well tolerated, does not cause metabolic disturbances and, apart from the typical dihydropyridine-type vascular adverse effects, e.g. flushing and ankle oedema, it does not cause any specific side effect[3]. The confirmation of its antihypertensive efficacy, along with its favourable haemodynamic profile and reversal of left ventricular hypertrophy, minimal effect on glucose and lipid metabolism, preservation of quality of life and good tolerability, makes isradipine a suitable drug for the treatment of most patients with mild to moderate hypertension[4]. Isradipine-induced acceleration of the Ca(v)1.2 current decay reflects enhanced fast voltage-dependent inactivation and not open channel block[2]. Isradipine in vitro attenuates beta amyloid oligomer toxicity by suppressing calcium influx into cytoplasm and by suppressing Ca(v)1.2 expression. Isradipine became bioavailable, lowered tau burden, and improved autophagy function in the brain[5]. Chronic isradipine treatment remodeled SNc DA neurons in a way that should not only diminish their vulnerability to mitochondrial challenges, but to autophagic stress as well[6].

Isradipine 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
NCT03538262 - Enrolling by invitation January 31, 2023 United States, New York ... 展开 >> CHeT Telemedicine (Site 363) Rochester, New York, United States, 14642 收起 <<
NCT00684489 Hypertension Not Applicable Completed - -
NCT01587742 - Completed - -

Isradipine 参考文献

[1]Tran PH, Tran TT, et al. Physical properties and in vivo bioavailability in human volunteers of isradipine using controlled release matrix tablet containing self-emulsifying solid dispersion. Int J Pharm. 2013 Jun 25;450(1-2):79-86.

[2]Berjukow S, Hering S. Voltage-dependent acceleration of Ca(v)1.2 channel current decay by (+)- and (-)-isradipine. Br J Pharmacol. 2001; 133(7):959‐966

[3]Hansson L. Isradipine in hypertension. Drugs. 1990; 40 Suppl 2:10‐14

[4]Brogden RN, Sorkin EM. Isradipine. An update of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in the treatment of mild to moderate hypertension. Drugs. 1995; 49(4):618‐649

[5]Anekonda TS, Quinn JF. Calcium channel blocking as a therapeutic strategy for Alzheimer's disease: the case for isradipine. Biochim Biophys Acta. 2011; 1812(12):1584‐1590

[6]Guzman JN, Ilijic E, Yang B, et al. Systemic isradipine treatment diminishes calcium-dependent mitochondrial oxidant stress. J Clin Invest. 2018; 128(6):2266‐2280

Isradipine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.93mL

5.39mL

2.69mL

Isradipine 技术信息

CAS号75695-93-1
分子式C19H21N3O5
分子量 371.387
别名 伊拉地平 ;PN 200-110
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(282.72 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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