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尼卡地平 /Nicardipine {[allProObj[0].p_purity_real_show]}

货号:A407345 同义名: YC-93 free base

Nicardipine is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage.

Nicardipine 化学结构 CAS号:55985-32-5
Nicardipine 化学结构
CAS号:55985-32-5
Nicardipine 3D分子结构
CAS号:55985-32-5
Nicardipine 化学结构 CAS号:55985-32-5
Nicardipine 3D分子结构 CAS号:55985-32-5
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Nicardipine 纯度/质量文件 产品仅供科研

货号:A407345 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

ERK,p38 MAPK,ROS 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 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 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。

Nicardipine 生物活性

靶点
  • Calcium Channel

描述 Nicardipine is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure. Nicardipine is a less potent Ca++ antagonist than nifedipine in atrial fibers and that the reduction of delayed potassium current, which occurs in a similar range of concentrations to the blockade of Isi, could also be involved in its therapeutic effects[3]. Nicardipine is more specific for vascular smooth muscle than for cardiac smooth muscle and for coronary than peripheral vasculature[4]. Nicardipine (10-12 to 10-8 M) decreased active tension and frequency of contraction in a concentration-dependent manner. The EC50 and EC95 of nicardipine in the inhibition of active tension of the uterine smooth muscle were 2.41 × 10-10 M and 3.06 × 10-7 M, respectively. The EC50 and EC95 of nicardipine in the inhibition of frequency of contraction of the uterine smooth muscle were 9.04 × 10-11 and 4.18 × 10-7 M, respectively[5]. CaMKII down-regulation/proteasome inhibition/cytosolic calcium up-regulation/cathepsin B activation/trypsinogen activation axis was present in pancreatic acinar cells injury under nicardipine treatment[6].

Nicardipine 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
NCT02286089 Age-related Macular Degenerati... 展开 >>on 收起 << Phase 1 Phase 2 Recruiting December 2019 United States, California ... 展开 >> Retina Vitreous Associates Medical Group Recruiting Los Angeles, California, United States, 900211 Contact: Janet Kurokouchi, B.Sc.    310-289-2478 ext 1243    JKurokouchi@laretina.com    Contact: Gerard Aquino, B.Sc.    310-289-2478 ext 1225    GAquino@laretina.com    Principal Investigator: David Boyer, MD          Byers Eye Institute, Stanford School of Medicine Recruiting Palo Alto, California, United States, 94303 Contact: Lisa Greer, MBA    650-725-9184    lgreer7@stanford.edu    Principal Investigator: Diana Do, Prof.          Retinal Consultants Medical Group Recruiting Sacramento, California, United States, 95819 Contact: Erin Nickerman    916-453-5429    nickermane@retinalMD.com    Contact: Whitney Lewis    916-453-5429    lewisw@retinalmd.com    Principal Investigator: David Telander, MD          West Coast Retina Medical Group, Inc Recruiting San Francisco, California, United States, 94109 Contact: Kaitlin E. Miani, BA    415-972-4607    kmiani@westcoastretina.com    Contact: C.          Principal Investigator: Richard McDonald, MD          Israel Hadassah Ein Kerem University Hospital Recruiting Jerusalem, Israel, 91120 Contact: Devora Marks Ohana    972-2-6776324    dryamdstudy@gmail.com    Principal Investigator: Tareq Jaouni, MD          Rabin Medical Center Recruiting Petah Tikva, Israel Contact: Vivi Dagan    972-3-9377199    eyeclinic@clalit.org.il    Principal Investigator: Rita Ehrlich, MD          Kaplan Medical Center Recruiting Rehovot, Israel Contact: Michal Scwartzberg    972-8-9441691    kaplaneye1@gmail.com    Principal Investigator: Haia Morori-Katz, MD          Tel Aviv Souraski Medical Center Recruiting Tel Aviv, Israel, 91121 Contact: Sagit Bechor    03-6974361    sagitba@tlvmc.gov.il    Principal Investigator: Adiel Barak, MD, Prof. 收起 <<
NCT02341560 Non Arteritic Anterior Ischemi... 展开 >>c Optic Neuropathy 收起 << Phase 2 Phase 3 Recruiting October 2020 -
NCT03077243 Carcinoma, Squamous Cell ... 展开 >> Head and Neck Neoplasms Oropharyngeal Neoplasms 收起 << Phase 2 Recruiting February 2025 United States, Florida ... 展开 >> University of Florida Recruiting Gainesville, Florida, United States, 32610 Contact: Robert Amdur, MD    352-265-0287    amdurr@shands.ufl.edu    University of Florida Proton Therapy Institute Recruiting Jacksonville, Florida, United States, 32206 Contact: Roi Dagan, MD    904-588-1445    rdagan@floridaproton.org    United States, North Carolina University of North Carolina at Chapel Hill, Department of Radiation Oncology Recruiting Chapel Hill, North Carolina, United States, 27599 Contact: Bhishamjit Chera, MD    984-974-0400    bchera@med.unc.edu    Contact: Rebecca Green, MSW    (984) 974-8440    rlgreen@med.unc.edu    Rex Healthcare Recruiting Raleigh, North Carolina, United States, 27607 Contact: Nathan Sheets, MD    919-784-1251    nathan.sheets@unchealth.unc.edu 收起 <<

Nicardipine 参考文献

[1]Huang BR, Chang PC, et al. Anti-neuroinflammatory effects of the calcium channel blocker nicardipine on microglial cells: implications for neuroprotection. PLoS One. 2014 Mar 12;9(3):e91167.

[2]Amenta F, Strocchi P, et al. Vascular and neuronal hypertensive brain damage: protective effect of treatment with nicardipine. J Hypertens Suppl. 1996 Oct;14(3):S29-35.

[3]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Nicardipine. 2017 Jan 11

[4]Pepine C. Nicardipine, a new calcium channel blocker: role for vascular selectivity. Clin Cardiol. 1989 May;12(5):240-6

[5]Kim DJ, Hwang MH, An TH, Jung KT. The relaxant effect of nicardipine on the isolated uterine smooth muscle of the pregnant rat. Anesth Pain Med (Seoul). 2019 Oct 31;14(4):429-433

[6]Xiao J, Lin H, Liu B, Jin J. CaMKII/proteasome/cytosolic calcium/cathepsin B axis was present in tryspin activation induced by nicardipine. Biosci Rep. 2019 Jul 2;39(7):BSR20190516

Nicardipine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.43mL

2.09mL

1.04mL

20.85mL

4.17mL

2.09mL

Nicardipine 技术信息

CAS号55985-32-5
分子式C26H29N3O6
分子量 479.525
别名 YC-93 free base
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,2-8°C

溶解度

DMSO: 105 mg/mL(218.97 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
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