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/ Ranolazine/雷诺嗪

Ranolazine/雷诺嗪 {[allProObj[0].p_purity_real_show]}

货号：A103291 同义名： CVT 303; RS 43285-003

Ranolazine 是一种钙摄取抑制剂，通过抑制钠钙通道发挥作用，对 Iₙₐ 和 Iₖᵣ 的 IC50 分别为 6 μM 和 12 μM，常用于慢性心绞痛的研究。

Ranolazine/雷诺嗪 化学结构 CAS号：95635-55-5
Ranolazine/雷诺嗪 化学结构
CAS号：95635-55-5
Ranolazine/雷诺嗪 3D分子结构
CAS号：95635-55-5
Ranolazine/雷诺嗪 化学结构 CAS号：95635-55-5
Ranolazine/雷诺嗪 3D分子结构 CAS号：95635-55-5
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Ranolazine/雷诺嗪 纯度/质量文件 产品仅供科研

货号：A103291 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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 ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

 		99%+
Dronedarone HCl ✔ 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 ✔ 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 +

N-type Ca2+ channel, IC50: 0.11 μM

L-type calcium channel, IC50: 12.2 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 ✔ 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。
产品名称 Sodium Channel ↓ 其他靶点 纯度
Tolperisone HCl ✔ 99%
Triamterene +++

ENaC, IC50: 4.5 μM

 		98%
Lamotrigine ✔ 98%
Vinpocetine ✔ 98%
Zonisamide ✔ 99%
Dronedarone HCl ✔ 95%
Procainamide HCl ✔ 99%
Bupivacaine HCl ✔ 99+%
Benzocaine ✔ 98%
Carbamazepine ++

Sodium channel, IC50: 131 μM

 		98%
Quinidine sulfate dihydrate ✔ 98%
Ibutilide fumarate ✔ 99%+
Dibucaine HCl ✔ 99+%
Mexiletine HCl ✔ 99%
Phenytoin ✔ 99+%
Camostat Mesylate +++

epithelial sodium channel (ENaC), IC50: 50 nM

 		99%+
Levobupivacaine ✔ 97+%
Oxcarbazepine +

sodium channel, IC50: 160 μM

 		98%
Amiloride HCl dihydrate ✔ 97%
Ambroxol 98+%
Primidone ✔ 99%
Propafenone ✔ 99%
A-803467 ++++

Na(V1.8) channel, IC50: 8 nM

 		99%+
Rufinamide ✔ 99%
Phenytoin sodium ✔ 98%
Proparacaine HCl +

Voltage-gated sodium channel, ED50: 3.4 mM

 		98+%
Amiloride HCl ✔ 98%
Riluzole ✔ 97%
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。

Ranolazine/雷诺嗪 生物活性

靶点

  • Calcium Channel
描述 Ranolazine is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[3]. Ranolazine antagonizes the ventricular repolarization changes caused by clofilium and suppresses clofilium-induced TdP (Torsade de Pointes) in rabbits[4]. Ranolazine potentiates the effects of ACEIs (angiotensin-converting enzyme inhibitor) and ARBs (angiotensin receptor blocker). Clinicians should monitor for this potentiation when initiating treatment with ranolazine and an ACEI or ARB[5]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor. Ranolazine reduces cellular acetyl-CoA content via inhibition of fatty acid beta-oxidation and activates pyruvate dehydrogenase. Ranolazine significantly reduces infarct size and cardiac troponin T release in rats subjected to left anterior descending coronary artery occlusion-reperfusion[6]. Ranolazine therapy may decrease A1C (andhemoglobin A1C) among patients with T2DM without an increase in hypoglycemia. For patients with T2DM (type 2 diabetes mellitus) and chronic stable angina, ranolazine may be of use given its utility in cardiovascular disease and benefit in A1C lowering[7].

Ranolazine/雷诺嗪 细胞实验

Cell Line
Concentration Treated Time Description References
501mel cells 50 µM or 100 µM Once per week Inhibited fatty acid oxidation and reduced the formation of resistant cells Nat Metab. 2023 Sep;5(9):1544-1562.
WM9 cells 50 µM or 100 µM Once per week Inhibited fatty acid oxidation and reduced the formation of resistant cells Nat Metab. 2023 Sep;5(9):1544-1562.
A375 cells 100 µM Inhibited fatty acid oxidation and delayed the emergence of acquired resistance to BRAF inhibitors (BRAFi) Nat Metab. 2023 Sep;5(9):1544-1562.
Human atrial CMs (AF patients) 10 μmol/L reduction of SR-Ca2+ leak Cardiovasc Res. 2015 Jul 1;107(1):184-96.
Murine atrial CMs 10 μmol/L inhibition of ATX-II-induced SR-Ca2+ leak Cardiovasc Res. 2015 Jul 1;107(1):184-96.
HEK cells (expressing NaV1.5) 50 μM 10 minutes Ranolazine reduced peak Na+ current by 37±5% and inhibited the mechanosensitivity of NaV1.5 induced by bath flow. Circulation. 2012 Jun 5;125(22):2698-706.
Murine ventricular cardiac myocytes 50 μM 10 minutes Ranolazine inhibited the flow-induced increase in peak Na+ current, reducing peak Na+ current by 68±3%. Circulation. 2012 Jun 5;125(22):2698-706.
Cardiomyocytes 1 μmol/L Ranolazine at low concentrations selectively blocks INaL without affecting peak INa, normalizing APD in SGK1-CA cardiomyocytes and reducing the occurrence of after-depolarizations (EADs and DADs). Circulation. 2012 Oct 30;126(18):2208-19.
Detergent extracted fiber bundles 10 μmol/L 15 minutes To assess the effect of Ranolazine on myofilament response to Ca2+ in DOCA-salt hearts. Results showed that Ranolazine reduced maximum tension and Ca2+ sensitivity, restoring them to levels similar to sham fibers. Circ Res. 2012 Mar 16;110(6):841-50.
Cardiomyocytes 10 μmol/L 10 minutes To evaluate the effect of Ranolazine on diastolic function in cardiomyocytes from DOCA-salt hypertensive model. Results showed that Ranolazine improved diastolic function, normalizing the relaxation time constant τ. Circ Res. 2012 Mar 16;110(6):841-50.
MDA-MB-231-Luc cells 50 μM 24 hours Inhibited Na V1.5 currents and reduced breast cancer cell invasiveness Mol Cancer. 2014 Dec 11;13:264.

Ranolazine/雷诺嗪 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Wild-type (WT) mice 10 μmol/L Inhibition of ATX-II-induced SR-Ca2+ leak Cardiovasc Res. 2015 Jul 1;107(1):184-96.
Mice DOCA-salt hypertensive model Intravenous injection 5 mg/kg Single dose followed by continuous infusion To evaluate the effect of Ranolazine on diastolic function in DOCA-salt hypertensive model. Results showed that Ranolazine improved diastolic function, reducing the slope of end-diastolic pressure-volume relationship (EDPVR) to sham levels. Circ Res. 2012 Mar 16;110(6):841-50.
Mice Scn5a S571E and S571A knock-in mouse models 20 mg/kg Single dose Ranolazine normalized isoproterenol-induced repolarization defects in S571E myocytes and reduced arrhythmia events in S571E mice in vivo. Circulation. 2015 Aug 18;132(7):567-77
Mice H/H mice 10 μM To investigate the effects of ranolazine on action potential duration, results showed that ranolazine slightly prolonged action potentials in both male and female ventricular myocytes, but no statistically significant difference was detected between genders. Cardiovasc Res. 2012 Aug 1;95(3):300-7

Ranolazine/雷诺嗪 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
NCT02425969 Grey-zone Fractional Flow Rese... 展开 >>rve Intermediate Coronary Lesions Stable Angina Coronary Physiology 收起 << Not Applicable Completed - United Kingdom ... 展开 >> Golden Jubilee National Hospital Glasgow, Dunbartonshire, United Kingdom, G81 4DY 收起 <<
NCT01703156 Low Risk Acute Coronary Syndro... 展开 >>me 收起 << Not Applicable Completed - United States, Oklahoma ... 展开 >> Veteran's Affairs Medical Center Oklahoma City, Oklahoma, United States, 73104 收起 <<
NCT01215253 - Completed - -

Ranolazine/雷诺嗪 参考文献

[1]Undrovinas AI, Belardinelli L, et al. Ranolazine improves abnormal repolarization and contraction in left ventricular myocytes of dogs with heart failure by inhibiting late sodium current. J Cardiovasc Electrophysiol. 2006 May;17 Suppl 1:S169-S177.

[2]Song Y, Shryock JC, et al. Antagonism by ranolazine of the pro-arrhythmic effects of increasing late INa in guinea pig ventricular myocytes. J Cardiovasc Pharmacol. 2004 Aug;44(2):192-9.

[3]Keating GM. Ranolazine: a review of its use as add-on therapy in patients with chronic stable angina pectoris. Drugs. 2013; 73(1):55‐73

[4]Wang WQ, Robertson C, Dhalla AK, Belardinelli L. Antitorsadogenic effects of ({+/-})-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3- (2-methoxyphenoxy) propyl] -1-piperazine (ranolazine) in anesthetized rabbits. J Pharmacol Exp Ther. 2008; 325(3):875‐881

[5]Marciniak TA, Serebruany V. Ranolazine, ACE Inhibitors, and Angiotensin Receptor Blockers. Am J Med. 2019; 132(12):e844‐e845

[6]Zacharowski K, Blackburn B, Thiemermann C. Ranolazine, a partial fatty acid oxidation inhibitor, reduces myocardial infarct size and cardiac troponin T release in the rat. Eur J Pharmacol. 2001; 418(1-2):105‐110

[7]Greiner L, Hurren K, Brenner M. Ranolazine and Its Effects on Hemoglobin A1C. Ann Pharmacother. 2016; 50(5):410‐415

Ranolazine/雷诺嗪 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.69mL

2.34mL

1.17mL

23.39mL

4.68mL

2.34mL

Ranolazine/雷诺嗪 技术信息

CAS号95635-55-5
分子式C24H33N3O4
分子量 427.54
SMILES Code C1=C(C(=CC=C1)OC)OCC(CN3CCN(CC(NC2=C(C=CC=C2C)C)=O)CC3)O
MDL No. MFCD00864690
别名 CVT 303; RS 43285-003
运输蓝冰
InChI Key XKLMZUWKNUAPSZ-UHFFFAOYSA-N
Pubchem ID 56959
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 105 mg/mL(245.59 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Ranolazine | 95635-55-5 | CVT 303 | RS 43285-003 | CVT303 | CVT-303 | Sodium Current/FAO Inhibitor | Membrane Transporter/Ion Channel | Neuronal Signaling | Sodium Channel | Calcium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ranolazine/雷诺嗪 纯度/质量文件 | Ranolazine/雷诺嗪 亚型比较 | Ranolazine/雷诺嗪 生物活性 | Ranolazine/雷诺嗪 临床数据 | Ranolazine/雷诺嗪 参考文献 | Ranolazine/雷诺嗪 实验方案 | Ranolazine/雷诺嗪 技术信息

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