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西尼地平 /Cilnidipine {[allProObj[0].p_purity_real_show]}

货号:A236779 同义名: FRC-8653

Cilnidipine is a dual L- and N-type calcium channel blocker with antihypertensive, sympatholytic and neuroprotective activity.

Cilnidipine 化学结构 CAS号:132203-70-4
Cilnidipine 化学结构
CAS号:132203-70-4
Cilnidipine 3D分子结构
CAS号:132203-70-4
Cilnidipine 化学结构 CAS号:132203-70-4
Cilnidipine 3D分子结构 CAS号:132203-70-4
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Cilnidipine 纯度/质量文件 产品仅供科研

货号:A236779 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。

Cilnidipine 生物活性

靶点
  • Calcium Channel

描述 Cilnidipine is a calcium channel blocker that blocks both L and N-type calcium channels and inhibits excessive release of norepinephrine from the sympathetic nerve ending. Cilnidipine which inhibits N-type calcium channels is more useful for patients with hypertension and diabetes mellitus from its effects on glucose and lipid metabolism and renal function[3]. Cilnidipine selectively reduced only L-type HVA I(Ca) at the low concentrations under 10(-7) and 10(-6) M. Cilnidipine blocked not only L- but also N-type HVA I(Ca). At the high concentration over 10(-6) M cilnidipine non-selectively blocked the T-type LVA and P/Q- and R-type HVA Ca2+ channels[4]. In the rat focal brain ischemia model, an anti-hypertensive and anti-sympathetic dose of cilnidipine could reduce the size of cerebral infarction, whereas an equipotent hypotensive dose of nilvadipine failed to affect it[5]. Cilnidipine is more effective than amlodipine at improving renal function and arterial stiffness in patients with essential hypertension[6]. Cilnidipine, a commercially available NTCC-blocking drug (N-type Ca2+-channels), prevents AF-induced autonomic, electrical and structural remodelling, along with associated AF (atrial fibrillation) promotion[7]. Cilnidipine has an advantage of causing less reflex tachycardia, less pedal edema and better control of proteinuria in comparison to L-type CCB (calcium channel blocker). By causing dilatation of efferent arteriole, it causes less damage to glomeruli and suppresses podocyte injury. Cilnidipine also increases insulin sensitivity. Cilnidipine as CCB can be a good choice in hypertensive patients with diabetes, chronic kidney disease and in patients developing pedal edema with other CCB[8].

Cilnidipine 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
NCT00541853 Kidney, Polycystic, Autosomal ... 展开 >>Dominant 收起 << Phase 4 Unknown November 2012 Japan ... 展开 >> Kyorin University School of Medicine Not yet recruiting Mitaka, Tokyo, Japan, 181-8611 Contact: Eiji Higashihara, M.D.    81+422475511 ext 5813    ehigashi@kyorin-u.ac.jp    Contact: Kikuo Nutahara, M.D.    81-422475511 ext 5815    kinuta@kyorin-u.ac.jp    Department of Urology, National Hospital Organaization Chiba-East Hospital Not yet recruiting Chiba, Chiba, Japan, 260-8712 Contact: Koichi Kamura, MD    81+432615171 ext 7607    kamura@cehpnet.com    Toranomon Hospital Kajigaya, Kidney center Not yet recruiting Kanagawa, Japan, 213-8587 Contact: Yoshifumi Ubara, MD    81+448775111 ext 6064    ubara@toranomon.gr.jp    Toranomon Hospital, Kidney center Not yet recruiting Tokyo, Japan, 105-8470 Contact: Kenmei Tkaichi, MD    81+335881111 ext 7065    takaichi@toranomon.gr.jp    Division of Kidney and Hypertension, Department of Internal Medicine, Jikei University School of Medicine Not yet recruiting Tokyo, Japan, 105-8471 Contact: Tatsuo Hosoya, MD    81+334331111 ext 3220    t-hosoya@jikei.ac.jp    Contact: Kazushige Hanaoka, MD    81+334331111 ext 3221    khanaoka@jikei.ac.jp    Department of Urology, Teikyo University, School of Medicine Not yet recruiting Tokyo, Japan, 173-8605 Contact: Shigeo Horie, MD    81+339641211    shorie@med.teikyo-u.ac.jp    Contact: Satoru Muto, MD    81+33964-1211    muto@med.teikyo-u.ac.jp 收起 <<
NCT02145104 Hypertension Phase 3 Completed - Korea, Republic of ... 展开 >> Seoul National University Bundang Hospital Seongnam-si, Kyung-gi, Korea, Republic of 收起 <<
NCT00890279 Kidney, Polycystic, Autosomal ... 展开 >>Dominant 收起 << Phase 2 Unknown November 2012 Japan ... 展开 >> Department of Medicine II, Hokkaido Univserity School of Medicine Recruiting Sapporo, Hokkaido, Japan, 0608638 Contact: Toshio Mochizuki, MD    +81117065915    mtoshi@med.hokudai.ac.jp    Principal Investigator: Toshio Mochizuki, MD          Toranomon Hospital Kajigaya, Kidney center Not yet recruiting Kawasaki, Kanagawa, Japan, 2138587 Contact: Yoshihumi Ubara, MD    +81448775111 ext 6064    ubara@toranomon.gr.jp    Principal Investigator: Yoshihumi Ubara, MD          Department of Medicine II, Nippon Medical School Not yet recruiting Bunkyo-ku, Tokyo, Japan, 1138602 Contact: Yasuhiko Iino, MD    +81338222131    iinoyasuhiko@nms.ac.jp    Principal Investigator: Yasuhiko Iino, MD          Department of Urology, Teikyo University School of Medicine Recruiting Itabashi-ku, Tokyo, Japan, 1738605 Contact: Shigeo Horie, MD    +81339642497    shorie@med.teikyo-u.ac.jp    Contact: Satoru Muto, MD    +81339642497    muto@med.teikyo-u.ac.jp    Principal Investigator: Shigeo Horie, MD          Toranomon Hospital, Kidney center Not yet recruiting Minato-ku, Tokyo, Japan, 1058470 Contact: Kenmei Takaichi, MD    +81335881111 ext 7065    takaichi@toranomon.gr.jp    Principal Investigator: Kenmei Takaichi, MD          Division of Kidney and Hypertension, Department of Internal Medicine, Jikei University School of Medicine Active, not recruiting Minato-ku, Tokyo, Japan, 1058471 Department of Urology, Kyorin University School of Medicine Not yet recruiting Mitaka, Tokyo, Japan, 1818611 Contact: Eiji HIgashihara, MD    81422475511    ehigashi@kyorin-u.ac.jp    Contact: Kikuo Nutahara, MD    81422475511    kinuta@kyorin-u.ac.jp    Principal Investigator: Eiji Higashihara, MD          Sub-Investigator: Kikuo Nutahara, MD          Department of Urology, National Hospital Organaization Chiba-East Hospital Not yet recruiting Chiba, Japan, 2608712 Contact: Koichi Kamura, MD    +81432615171 ext 7607    kamura@cehpnet.com    Principal Investigator: Koichi Kamura, MD          Division of Clinical Nephrology and Rheumatology, Niigata University Graduate School of Medical and Dental Sciences Not yet recruiting Niigata, Japan, 9518510 Contact: Ichiei Narita, MD    +813252272193    naritai@med.niigata-u.ac.jp    Principal Investigator: Ichiei Narita, MD 收起 <<

Cilnidipine 参考文献

[1]Takahara A, Fujita S, et al. Neuronal Ca2+ channel blocking action of an antihypertensive drug, cilnidipine, in IMR-32 human neuroblastoma cells. Hypertens Res. 2003 Sep;26(9):743-7.

[2]Shiomi T, Tsutsui H, et al. Pioglitazone, a peroxisome proliferator-activated receptor-gamma agonist, attenuates left ventricular remodeling and failure after experimental myocardial infarction. Circulation. 2002 Dec 10;106(24):3126-32.

[3]Masuda T, Ogura MN, Moriya T, et al. Beneficial effects of L- and N-type calcium channel blocker on glucose and lipid metabolism and renal function in patients with hypertension and type II diabetes mellitus. Cardiovasc Ther. 2011;29(1):46‐53

[4]Murai Y, Uneyama H, Ishibashi H, Takahama K, Akaike N. Preferential inhibition of L- and N-type calcium channels in the rat hippocampal neurons by cilnidipine. Brain Res. 2000;854(1-2):6‐10

[5]Takahara A, Konda T, Enomoto A, Kondo N. Neuroprotective effects of a dual L/N-type Ca(2+) channel blocker cilnidipine in the rat focal brain ischemia model. Biol Pharm Bull. 2004;27(9):1388‐1391

[6]Morimoto S, Yano Y, Maki K, Iwasaka T. Renal and vascular protective effects of cilnidipine in patients with essential hypertension. J Hypertens. 2007;25(10):2178‐2183

[7]Tajiri K, Guichard JB, Qi X, et al. An N-/L-type calcium channel blocker, cilnidipine, suppresses autonomic, electrical, and structural remodelling associated with atrial fibrillation. Cardiovasc Res. 2019;115(14):1975‐1985

[8]Shete MM. Cilnidipine: Next Generation Calcium Channel Blocker. J Assoc Physicians India. 2016;64(4):95‐99

Cilnidipine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.15mL

2.03mL

1.02mL

20.30mL

4.06mL

2.03mL

Cilnidipine 技术信息

CAS号132203-70-4
分子式C27H28N2O7
分子量 492.52
别名 FRC-8653
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,Room Temperature

溶解度

DMSO: 105 mg/mL(213.19 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

5% DMSO+corn oil 7 mg/mL

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