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Ranolazine

Ranolazine

产品编号 T6633   CAS 95635-55-5
别名: 雷诺嗪, CVT 303, Ranexa, RS 43285-003

Ranolazine (RS 43285-003) 具有抗心绞痛和抗缺血的功效,通过抑制内向钠电流的后期作用 (对INa 和IKr 的IC50值分别为 6 μM 和 12 μM) 发挥作用,而不会影响心率或血压。Ranolazine 还是脂肪酸氧化 (FAO) 的部分抑制剂。

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Ranolazine Chemical Structure
Ranolazine, CAS 95635-55-5
规格 价格/CNY 货期 数量
10 mg ¥ 192 现货
25 mg ¥ 335 现货
50 mg ¥ 513 现货
100 mg ¥ 742 现货
200 mg ¥ 1,136 现货
500 mg ¥ 1,854 现货
1 mL * 10 mM (in DMSO) ¥ 148 现货
其他形式的 Ranolazine:
产品目录号及名称: Ranolazine (T6633)
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纯度: 98.2%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Ranolazine (RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina. It affects the sodium-dependent calcium channels during myocardial ischemia in rabbits by altering the intracellular sodium level.
靶点活性 IKr:12 μM (IC50), INa:6 μM (IC50)
体外活性 In the absence and presence of IK-blocking drugs, when late INa is increased, Ranolazine inhibits the late component of INa and attenuates prolongation of action potential duration. Ranolazine (10 mM) reduces by 89% of the 13.6-fold increase in variability of APD caused by 10 nM ATX-II. Ranolazine is found to bind more tightly to the inactivated state than the resting state of the sodium channel underlying I(NaL), with apparent dissociation constants K(dr)=7.47 mM and K(di)=1.71 mM, respectively. Ranolazine(5 mM and 10 mM) reversibly shortens the duration of TCs and abolishes the after contraction.
体内活性 In dog left ventricular myocytes, Ranolazine significantly and reversibly stimulate the action potential duration (APD) of shortened myocytes at 0.5 or 0.25 Hz in a concentration-dependent manner. In rat hearts, Ranolazine (10 mM) significantly increased 1.5-fold to 3-fold under glucose oxidation conditions. Ranolazine (10 mM) also increased glucose oxidation (high calcium, low FA; 15 ml/min) in Langendorff hearts in normoxic rats. Ranolazine significantly improves the function of the reperfused ischemic working heart, which is associated with a significant increase in glucose oxidation function.
激酶实验 In vitro kinase assay for CDK1 and Aurora kinases:CDK1 kinase activity is tested by the CDK1/cyclin B complex purified from baculovirus to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylated in vivo by CDK1. Inhibition of CDK1 activity is measured by observing a decreased amount of 33P-γ-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO4, 1 mM DTT, 1% DMSO, 0.25 μM peptide, 0.1 μCi per well 33P-γ-ATP, and 5 μM ATP in the presence or absence of various concentrations of JNJ-7706621 and incubated at 30 °C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. IC50 is determined by Linear regression analysis of the percent inhibition by JNJ-7706621.The Aurora kinase activity is measured with 10 μM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif.
别名 雷诺嗪, CVT 303, Ranexa, RS 43285-003
分子量 427.54
分子式 C24H33N3O4
CAS No. 95635-55-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 16 mg/mL (37.4 mM)

DMSO: 80 mg/mL (187.1 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.339 mL 11.6948 mL 23.3896 mL 58.4741 mL
5 mM 0.4678 mL 2.339 mL 4.6779 mL 11.6948 mL
10 mM 0.2339 mL 1.1695 mL 2.339 mL 5.8474 mL
20 mM 0.1169 mL 0.5847 mL 1.1695 mL 2.9237 mL
DMSO 50 mM 0.0468 mL 0.2339 mL 0.4678 mL 1.1695 mL
100 mM 0.0234 mL 0.1169 mL 0.2339 mL 0.5847 mL

计算器

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分子量计算器
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参考文献

1. Undrovinas AI, et al. J Cardiovasc Electrophysiol,2006, 17 Suppl 1, S169-S177. 2. Song Y, et al. J Cardiovasc Pharmacol,2004, 44(2), 192-199. 3. Baptista T, et al. Circulation,1996, 93(1), 135-142.

文献引用

1. Lenaeus M, Gamal El-Din T M, Tonggu L, et al.Structural basis for inhibition of the cardiac sodium channel by the atypical antiarrhythmic drug ranolazine.Nature Cardiovascular Research.2023: 1-8.
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相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 抗癌上市药物库 肝脏毒性化合物库 临床期小分子药物库 抗糖尿病库 抗COVID-19化合物库 代谢化合物库 FDA 上市药物库 抗高血压化合物库

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Ranolazine 95635-55-5 Membrane transporter/Ion channel Metabolism Calcium Channel Sodium Channel 雷诺嗪 CVT303 Na+ channels Ca2+ channels inhibit CVT-303 CVT 303 Inhibitor Ranexa RS 43285-003 Na channels Ca channels inhibitor

 

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