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

货号:A103291 同义名: CVT 303;RS 43285-003

Ranolazine inhibits calcium uptake via the sodium/calcium channel, is used to treat chronic angina.

Ranolazine 化学结构 CAS号:95635-55-5
Ranolazine 化学结构
CAS号:95635-55-5
Ranolazine 3D分子结构
CAS号:95635-55-5
Ranolazine 化学结构 CAS号:95635-55-5
Ranolazine 3D分子结构 CAS号:95635-55-5
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Ranolazine 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]}
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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

ROS,ERK,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。
产品名称 Sodium Channel 其他靶点 纯度
Tolperisone HCl 99%
Lamotrigine 98%
Vinpocetine 98%
Zonisamide 98%
Dronedarone Hydrochloride 95%
Procainamide hydrochloride 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%
Ambroxol 98+%
Primidone 99%
Propafenone 99%
A-803467 ++++

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

99%+
Rufinamide 99%
Phenytoin sodium 98%
Proparacaine Hydrochloride +

Voltage-gated sodium channel, ED50: 3.4 mM

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 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 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 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 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 技术信息

CAS号95635-55-5
分子式C24H33N3O4
分子量 427.536
别名 CVT 303;RS 43285-003
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,Room Temperature

溶解度

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

动物实验配方
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