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/ Manidipine Dihydrochlorid

盐酸马尼地平 /Manidipine Dihydrochlorid {[allProObj[0].p_purity_real_show]}

货号：A108830 同义名： CV-4093;Manidipine 2HCl

Manidipine 2HCl is a L/T-type calcium channel blocker for Ca2+ current with IC50 of 2.6 nM.

Manidipine Dihydrochlorid 化学结构 CAS号：89226-75-5
Manidipine Dihydrochlorid 化学结构
CAS号：89226-75-5
Manidipine Dihydrochlorid 3D分子结构
CAS号：89226-75-5
Manidipine Dihydrochlorid 化学结构 CAS号：89226-75-5
Manidipine Dihydrochlorid 3D分子结构 CAS号：89226-75-5
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Manidipine Dihydrochlorid 纯度/质量文件 产品仅供科研

货号：A108830 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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 ++

hCaV3.2, IC50: 110 nM

hCaV3.1, IC50: 50 nM

 		99%+
Dronedarone Hydrochloride ✔ 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

 		98%
Efonidipine HCl monoethanolate ✔ 98%
Cinnarizine ✔ 98%
SEA0400 ++

NCX, IC50: 33 nM

 		ERK,ROS,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。

Manidipine Dihydrochlorid 生物活性

靶点

  • Calcium Channel

    Calcium channel, IC50:2.6 nM
描述 Manidipine (Dihydrochloride) is a lipophilic, third-generation, highly vasoselective, dihydropyridine (DHP) calcium channel antagonist, which, when given on a once-daily basis, effectively reduces blood pressure (BP) in patients with mild-to-moderate essential hypertension. Diabetic patients and very elderly patients with mild-to-moderate hypertension also respond favourably to treatment with manidipine[3]. Manidipine shows long-lasting calcium channel-blocking action in vascular smooth muscle cells and antihypertensive actions in various types of hypertensive models. The drug has high selectivity for resistance vessels, dilates renal vasculature, and inhibits renal vascular constrictions induced by norepinephrine and angiotensin II in spontaneously hypertensive rats. It increases renal blood flow and has a prominent natriuretic action without changing glomerular filtration rate. Furthermore, manidipine prevents the development of cerebrovascular lesions and inhibits the progression of vascular damage in the brain and kidneys of stroke-prone spontaneously hypertensive rats. The drug also inhibits a proliferative response of the intima to balloon catheter-induced injury in the carotid arteries of spontaneously diabetic rats without affecting plasma lipids or blood pressure[4]. In human macrophages THP-1, treatment with different cytokines was able to stimulate by about 3-folds the release of IL-6 (interleukin-6) and Manidipine 1 microM showed a 25% inhibition on TNF-alpha-induced IL-6 secretion. In these cells, a combined treatment with multiple cytokines, induced IL-6 production of about 6-folds and Manidipine was able to reduce such inflammatory response by 30%[5]. Manidipine plus delapril is a fixed-dose combination of a third-generation dihydropyridine calcium antagonist and an angiotensin-converting enzyme inhibitor, which is effective in mild-to-moderately hypertensive patients with an inadequate response to monotherapy[6]. The antiviral activity of MND (Manidipine Dihydrochloride) is specific for HCMV (human cytomegalovirus) over different both DNA and RNA viruses. Further experiments in HCMV-infected cells testing the effects of MND on viral DNA synthesis and viral proteins expression revealed that it halts the progression of the virus cycle prior to viral DNA replication and E genes expression, but after IE proteins expression[7].

Manidipine Dihydrochlorid 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
NCT00157586 Type 2 Diabetes Phase 3 Completed - Italy ... 展开 >> ASL of Ponte San Pietro - Diabetologic Unit Ponte San Pietro, Bergamo, Italy, 24036 Clinical Research Center for Rare Diseases Ranica, Bergamo, Italy, 24020 Hospital of Romano di Lombardia - Diabetologic Unit Romano di Lombardia, Bergamo, Italy, 24058 Hospital " Bolognini " - Medicine Unit Seriate, Bergamo, Italy, 24068 Hospital " Treviglio Caravaggio" - Diabetologic Unit Treviglio, Bergamo, Italy, 24128 Humanitas Institute - Endocrinology and Diabetologic Unit Rozzano, Milano, Italy, 20089 Hospital "Ospedali Riuniti di Bergamo" - Diabetologic Unit Bergamo, Italy, 24128 Slovenia Department of Endocrinolgy, Diabetes and Metabolic Disease - University Medical Center Lubiana, Slovenia 收起 <<
NCT03106597 Hypertension Phase 4 Recruiting December 10, 2018 Korea, Republic of ... 展开 >> Yonsei University Severance Hospital Recruiting Seoul, Korea, Republic of, 03722 Contact: Sang Hak Lee, MD, PhD    82-10-5472-6911    shl1106@yuhs.ac    Sub-Investigator: Sang Hak Lee, MD, PhD          Korea University Guro Hospital Recruiting Seoul, Korea, Republic of, 08308 Contact: Seung-hoe Song, MBE    82-2-2626-1635    ssessong@korea.ac.kr    Contact: Da-in Lee    82-2-2626-2279    0124dain@gmail.com    Yonsei University Wonju Hospital Recruiting Wonju, Korea, Republic of, 26426 Contact: Jang Young Kim, PhD          Contact    82-10-5360-0463    kimjy@yonsei.ac.kr    Sub-Investigator: Jang Young Kim, PhD 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 <<

Manidipine Dihydrochlorid 参考文献

[1]Tohse N, Takeda Y, Kanno M. Voltage-dependent modulation of L-type Ca2+ current by manidipine in guinea-pig heart cells. Eur J Pharmacol. 1993 Nov 9;249(2):231-3.

[2]Pfaffendorf M, Mathy MJ, van Zwieten PA. Effects of manidipine and other calcium antagonists on rat renal arcuate arteries. Am Heart J. 1993 Feb;125(2 Pt 2):571-7.

[3]Roca-Cusachs A, Triposkiadis F. Antihypertensive effect of manidipine. Drugs. 2005; 65 Suppl 2:11‐19

[4]Nagaoka A. Pharmacologic characteristics of a new calcium antagonist, manidipine: beneficial effects on renal circulation and vascular changes. Am Heart J. 1993; 125(2 Pt 2):560‐565

[5]Costa S, Zimetti F, Pedrelli M, Cremonesi G, Bernini F. Manidipine reduces pro-inflammatory cytokines secretion in human endothelial cells and macrophages. Pharmacol Res. 2010; 62(3):265‐270

[6]Coca A. Manidipine plus delapril in patients with Type 2 diabetes and hypertension: reducing cardiovascular risk and end-organ damage. Expert Rev Cardiovasc Ther. 2007; 5(2):147‐159

[7]Mercorelli B, Luganini A, Celegato M, Palù G, Gribaudo G, Loregian A. Repurposing the clinically approved calcium antagonist manidipine dihydrochloride as a new early inhibitor of human cytomegalovirus targeting the Immediate-Early 2 (IE2) protein. Antiviral Res. 2018; 150:130‐136

Manidipine Dihydrochlorid 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.46mL

0.29mL

0.15mL

7.31mL

1.46mL

0.73mL

14.63mL

2.93mL

1.46mL

Manidipine Dihydrochlorid 技术信息

CAS号89226-75-5
分子式C35H40Cl2N4O6
分子量 683.621
别名 CV-4093;Manidipine 2HCl;Manidipine dihydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C
溶解度

DMSO: 50 mg/mL(73.14 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

2% DMSO+30% PEG 300+water 2 mg/mL

Tags: Manidipine | 89226-75-5 | CV-4093 | CV4093 | CV 4093 | Calcium Channel Antagonist | Membrane Transporter/Ion Channel | Neuronal Signaling | NF-κB | Calcium Channel | NF-κB | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Manidipine Dihydrochlorid 纯度/质量文件 | Manidipine Dihydrochlorid 亚型比较 | Manidipine Dihydrochlorid 生物活性 | Manidipine Dihydrochlorid 临床数据 | Manidipine Dihydrochlorid 参考文献 | Manidipine Dihydrochlorid 实验方案 | Manidipine Dihydrochlorid 技术信息

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