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/ Lercanidipine/乐卡地平

Lercanidipine/乐卡地平 {[allProObj[0].p_purity_real_show]}

货号：A381766

Lercanidipine 是一种第三代、亲脂性、可穿透血脑屏障、口服活性的二氢吡啶类钙通道阻滞剂，pIC50 为 7.74（从微摩尔浓度转换）。Lercanidipine 具有持久的降压作用，并具有肾脏和神经保护特性，还具有抗氧化、抗炎和抗凋亡特性。Lercanidipine 用于心血管和神经系统研究。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Lercanidipine/乐卡地平 化学结构 CAS号：100427-26-7
Lercanidipine/乐卡地平 化学结构
CAS号：100427-26-7
Lercanidipine/乐卡地平 3D分子结构
CAS号：100427-26-7
Lercanidipine/乐卡地平 化学结构 CAS号：100427-26-7
Lercanidipine/乐卡地平 3D分子结构 CAS号：100427-26-7
规格 价格 会员价 库存 数量
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Lercanidipine/乐卡地平 纯度/质量文件 产品仅供科研

货号：A381766 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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更多 >
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 ✔ 99%
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 HCl ✔ 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 ✔ PKA,Rho 98%
ML-9 ✔ MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

 		95%
Lomerizine 2HCl ✔ 98%
Efonidipine ✔ 98%
Levamlodipine ✔ 98%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

 		97%
Isradipine ✔ 98%
Lacidipine ✔ 98%
Lercanidipine ✔ 99%
Loureirin B ✔ Potassium Channel 99%+
Tetracaine HCl ✔ 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

 		99%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

 		98%
Nicardipine ✔ 99%
Wilforgine ✔ 98+%
Econazole ✔ 99%+
Ginsenoside Rd ✔ NF-κB 98%
Fendiline HCl ✔ 98+%
Mesaconitine ✔ 98%
Tetrandrine ✔ 95%
Nifedipine ✔ 98%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

 		95%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

 		95+%
Azelnidipine ✔ 97%
Levetiracetam ✔ 98%
Nimodipine ✔ 95%
Benidipine HCl ✔ 98%
Pinaverium bromide ✔ 98%
Pranidipine ✔ 99%
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

 		95%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

 		97%
Cilnidipine ✔ 99%
Cinepazide Maleate ✔ 99% (HPLC)
Terfenadine ✔ 98%
YM-58483 ✔ 99%+
Amiloride HCl ✔ 98%
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。
产品名称 NF-κB ↓ 其他靶点 纯度
Ammonium pyrrolidine-1-carbodithioate ✔ 98%
QNZ ++++

NF-κB, IC50: 11 nM

 		99%+
Sodium 4-Aminosalicylate Dihydrate ✔ 98%
Sodium Salicylate ✔ 95%
Parthenolide ✔ p53 97% HPLC
JSH-23 +

NF-κB, IC50: 7.1 μM

 		98%
Phenethyl caffeate ✔ 98%
Andrographolide ✔ 98+%
Curcumin ✔ HDAC,Nrf2 98%
SC75741 +++

NF-κB, EC50: 200 nM

 		99%+
CBL0137 HCl ++

NF-κB, EC50: 0.47 μM

 		p53 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 p38 MAPK ↓ p38α ↓ p38β ↓ 其他靶点 纯度
BMS-582949 +++

p38 MAPK, IC50: 13 nM

 		98%
Adezmapimod 99%+
Pexmetinib ✔ Tie-2 99%+
Skepinone-L ++++

p38α, IC50: 5 nM

 		98%
Doramapimod ++++

p38α, IC50: 38 nM

p38α, Kd: 0.1 nM

 		99%+
VX-702 99%+
Ralimetinib dimesylate ++++

p38α, IC50: 7 nM

 		98%
SB 202190 ++

p38α, IC50: 50 nM

 		++

p38β, IC50: 100 nM

 		99%+
Losmapimod ++++

p38α, pKi: 8.1

 		+++

p38β, pKi: 7.6

 		99%+
Neflamapimod +++

p38α, IC50: 10 nM

 		+

p38β, IC50: 220 nM

 		99%+
PH-797804 ++

p38α, IC50: 26 nM

 		+

p38β, IC50: 102 nM

 		99%
TAK-715 ++++

p38α, IC50: 7.1 nM

 		+

p38β, IC50: 0.20 μM

 		99%+
SB 239063 ++

p38α, IC50: 44 nM

 		++

p38β, IC50: 44 nM

 		99%+
Pamapimod +++

p38α, IC50: 0.014 μM

 		+

p38β, IC50: 0.48 μM

 		98%+
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。

Lercanidipine/乐卡地平 生物活性

靶点

  • Calcium Channel
描述 Lercanidipine is a calcium channel blocker of the dihydropyridine class.

Lercanidipine/乐卡地平 细胞实验

Cell Line
Concentration Treated Time Description References
Vero cells Vero cells Screening for LUJV entry inhibitors Front Microbiol. 2021 Dec 2;12:793519.
Chang (normal liver cells) Chang (normal liver cells) 24 h Lercanidipine did not significantly increase the cytotoxicity of Bortezomib in normal cells Int J Mol Sci. 2019 Dec 4;20(24):6112.
MCF-10A (normal breast cells) MCF-10A (normal breast cells) 24 h Lercanidipine did not significantly increase the cytotoxicity of Bortezomib in normal cells Int J Mol Sci. 2019 Dec 4;20(24):6112.
RPMI-8226 (multiple myeloma cells) RPMI-8226 (multiple myeloma cells) 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
BxPC-3 (pancreatic cancer cells) BxPC-3 (pancreatic cancer cells) 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
NCI-H460 (lung cancer cells) NCI-H460 (lung cancer cells) 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
SNU-668 (stomach cancer cells) SNU-668 (stomach cancer cells) 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
SNU-475 (liver cancer cells) SNU-475 (liver cancer cells) 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
MDA-MB 435S (breast cancer cells) MDA-MB 435S (breast cancer cells) 24 h Lercanidipine enhances the cytotoxicity of Bortezomib in cancer cells, inducing paraptosis-associated cell death Int J Mol Sci. 2019 Dec 4;20(24):6112.
Primary lung cancer cells Primary lung cancer cells Inhibited the expression of PD-L1 Front Pharmacol. 2021 Jan 13;11:539261.
NCI-H460 cells NCI-H460 cells Inhibited the transcriptional levels of PD-L1 Front Pharmacol. 2021 Jan 13;11:539261.
NCI-H1299 cells NCI-H1299 cells Inhibited the transcriptional levels of PD-L1 Front Pharmacol. 2021 Jan 13;11:539261.
A172GSC cells A172GSC cells Inhibited GLT8D1 expression, reduced CD133 and β-catenin protein stability Cell Death Differ. 2022 Sep;29(9):1834-1849.
U251GSC cells U251GSC cells Inhibited GLT8D1 expression, reduced CD133 and β-catenin protein stability Cell Death Differ. 2022 Sep;29(9):1834-1849.
GBM1 cells GBM1 cells Inhibited GLT8D1 expression, reduced CD133 and β-catenin protein stability Cell Death Differ. 2022 Sep;29(9):1834-1849.
GSC11 cells GSC11 cells Inhibited GLT8D1 expression, reduced CD133 and β-catenin protein stability Cell Death Differ. 2022 Sep;29(9):1834-1849.
OC-1 cells OC-1 cells To evaluate the antioxidative effect of Lercanidipine on OC-1 cell viability, results showed that 0.3 to 2.5 µM Lercanidipine significantly enhanced cellular viability Antioxidants (Basel). 2024 Mar 7;13(3):327.
CHO cells (expressing Ca v1.2b subunit) CHO cells (expressing Ca v1.2b subunit) To study the inhibitory effect of (S)-lercanidipine on vascular Ca v1.2b subunit, showing IC50=1.8×10^-8 M, Hill coefficient nH=0.8, indicating higher selectivity for the vascular isoform. Br J Pharmacol. 2004 May;142(2):275-84.
CHO cells (expressing Ca v1.2a subunit) CHO cells (expressing Ca v1.2a subunit) To study the inhibitory effect of (S)-lercanidipine on cardiac Ca v1.2a subunit, showing IC50=3.3×10^-8 M, Hill coefficient nH=2.3, indicating overlap between agonistic and antagonistic effects. Br J Pharmacol. 2004 May;142(2):275-84.

Lercanidipine/乐卡地平 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Xenograft tumor models Tail vein injection 5 mg/kg Twice every week for four weeks Suppressed tumor growth, reduced GLT8D1 and CD133 expression, increased apoptosis markers Cell Death Differ. 2022 Sep;29(9):1834-1849.
White New Zealand rabbits Atherosclerotic lesions induced by cholesterol feeding Subcutaneous injection 0.3, 1, and 3 mg/kg Once a week for 10 weeks Significantly reduced intimal hyperplasia and aortic fatty streak area in a dose-dependent manner Br J Pharmacol. 1998 Dec;125(7):1471-6
C57BL/6J mice Noise-induced hearing loss model Intraperitoneal injection 6 mg/kg 1 hour before noise exposure and once daily on days 1, 2, and 3 post-exposure To investigate the protective effect of Lercanidipine against noise-induced hearing loss, results showed that Lercanidipine significantly attenuated the elevation of hearing thresholds and preserved OHC survival in the basal turn Antioxidants (Basel). 2024 Mar 7;13(3):327.

Lercanidipine/乐卡地平 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
NCT00424801 Microvascular Angina ... 展开 >> Hypertension 收起 << Not Applicable Terminated(Due to recent findi... 展开 >>ngs relating MRI contrast to nephrogenic systemic fibrosis) 收起 << December 2008 Denmark ... 展开 >> Aarhus Hospital Aarhus, Denmark, 8000 收起 <<
NCT00741585 Essential Hypertension ... 展开 >> Cardiovascular Disease Stroke Chronic Kidney Disease 收起 << Phase 4 Completed - Spain ... 展开 >> CS Friol Friol, Lugo, Spain, 27220 CS Baiona Baiona, Pontevedra, Spain, 36300 CS Bueu Bueu, Pontevedra, Spain, 36930 CS A Estrada La Estrada, Pontevedra, Spain, 26680 CS A Guarda La Guardia, Pontevedra, Spain, 36780 CS Valmiñor Nigran, Pontevedra, Spain, 36250 CS Panxón Nigrán, Pontevedra, Spain, 36340 CS Tomiño Tomiño, Pontevedra, Spain, 36200 Bioengineering & Chronobilogy Labs., University of Vigo Vigo, Pontevedra, Spain, 36200 Hospital do Meixoeiro Vigo, Pontevedra, Spain, 36200 CS Calle Cuba Vigo, Pontevedra, Spain, 36202 CS A Doblada Vigo, Pontevedra, Spain, 36205 CS Coia Vigo, Pontevedra, Spain, 36209 CS Sardoma Vigo, Pontevedra, Spain, 36214 CS Teis Vigo, Pontevedra, Spain, 36216 CS Vilaboa Vilaboa, Pontevedra, Spain, 36141 CS San Roque Vilagarcía De Arousa, Pontevedra, Spain, 36600 CS Fingoi Lugo, Spain, 27002 Complexo Hospitalario Universitario de Ourense Orense, Spain, 32005 CS Lerez Pontevedra, Spain, 36156 收起 <<
NCT02594410 Hypertension Phase 4 Completed - China ... 展开 >> Fuwai Hospital Beijing, China 收起 <<

Lercanidipine/乐卡地平 参考文献

[1]Selvaraj N, Adhimoolam M, et al. Neuroprotective Effect of Lercanidipine- A Novel Calcium Channel Blocker in Albino Mice. J Clin Diagn Res. 2015 Nov;9(11):FF01-5.

[2]Cao TS, Huynh VM, et al. Effects of lercanidipine versus amlodipine in hypertensive patients with cerebral ischemic stroke. Curr Med Res Opin. 2015 Jan;31(1):163-70.

Lercanidipine/乐卡地平 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.63mL

0.33mL

0.16mL

8.17mL

1.63mL

0.82mL

16.35mL

3.27mL

1.63mL

Lercanidipine/乐卡地平 技术信息

CAS号100427-26-7
分子式C36H41N3O6
分子量 611.73
SMILES Code O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OC(C)(C)CN(CCC(C3=CC=CC=C3)C4=CC=CC=C4)C
MDL No. MFCD00867978
别名
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 105 mg/mL(171.65 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

Tags: Lercanidipine | 100427-26-7 | Membrane Transporter/Ion Channel | Neuronal Signaling | Apoptosis | Immunology/Inflammation | NF-κB | Metabolic Enzyme/Protease | MAPK/ERK Pathway | Calcium Channel | Apoptosis | Reactive Oxygen Species | p38 MAPK | NF-κB | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lercanidipine/乐卡地平 纯度/质量文件 | Lercanidipine/乐卡地平 亚型比较 | Lercanidipine/乐卡地平 生物活性 | Lercanidipine/乐卡地平 临床数据 | Lercanidipine/乐卡地平 参考文献 | Lercanidipine/乐卡地平 实验方案 | Lercanidipine/乐卡地平 技术信息

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