Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vipadenant (CEB-4520) 是一种腺苷受体拮抗剂,抑制 A2A 和 A1 活性的 Ki 值分别为 1.3 和 68 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 768 | 现货 | ||
2 mg | ¥ 1,130 | 现货 | ||
5 mg | ¥ 1,790 | 现货 | ||
10 mg | ¥ 2,830 | 现货 | ||
25 mg | ¥ 4,690 | 现货 | ||
50 mg | ¥ 6,720 | 现货 | ||
100 mg | ¥ 9,120 | 现货 | ||
500 mg | ¥ 18,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,920 | 现货 |
产品描述 | Vipadenant (CEB-4520)(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM). |
靶点活性 | adenosine A1:69 nM(Ki), adenosine A2a:1.3 nM(Ki) |
体内活性 | Vipadenant (0.3-30 mg/kg) produces a reduction in catalepsy in a dose-dependent manner. Vipadenant (10 mg/kg) does not produce any statistically significant dyskinetic episodes in 6-OHDA-lesioned rats during a 19-day dosing regimen[1]. In the mouse and rat haloperidol-induced hypolocomotion models, vipadenant has a minimum effective dose of 0.1 and 1 mg/kg, respectively. Vipadenant (3 and 10 mg/kg, p.o.) can increase contralateral rotations in 6-OHDA lesioned rats[2]. |
激酶实验 | Peptide substrate phosphorylation assays with GST-Abl kinase domains: The effect of AP24534 (0-320 nM) on GST-Abl kinase activity is assessed by using a synthetic peptide substrate (Abltide: EAIYAAPFAKKK). Assays are carried out at 30 °C for 15 min in 25 μL reaction mixture: 8 mM MOPS (pH 7), 0.2 mM EDTA, 50 μM Abltide, 30 mM MgCl2, 10 mM β-glycerol phosphate, 1 mM EGTA, 0.002% Brij-35, 0.4 mM DTT, 0.2 mg/mL BSA, 0.4 mM sodium orthovanadate, 10 nM WT or mutant GST-Abl kinase, and 100 μM ATP/γ-32[P]ATP (5000 cpm/pmol). Reactions are terminated by transferring a portion of the reaction mixture onto a p81 phosphocellulose filter and immersing in 0.75% phosphoric acid. Filters are washed 3 times in 0.75% phosphoric acid, rinsed in acetone, and air dried; phosphate incorporation is determined by scintillation counting. All results are corrected for background binding to the filters, as determined by omitting peptide substrate from the kinase reaction. Time course experiments to establish the linear range of enzymatic activity precedes kinase assays. |
别名 | CEB-4520, BIIB-014 |
分子量 | 321.34 |
分子式 | C16H15N7O |
CAS No. | 442908-10-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 31 mg/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。
Vipadenant 442908-10-3 GPCR/G Protein Neuroscience Adenosine Receptor CEB4520 BIIB 014 BIIB014 inhibit CEB 4520 Inhibitor P1 receptor CEB-4520 BIIB-014 inhibitor