Cilnidipine is a dual L- and N-type calcium channel blocker with antihypertensive, sympatholytic and neuroprotective activity.
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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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |