Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 16 mg/mL (37.4 mM)
DMSO: 80 mg/mL (187.1 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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