化合物Vipadenant T2373

Product Introduction
Bioactivity


英文名: Vipadenant

描述: 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。

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.

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].

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

溶解度: DMSO : 31 mg/mL


关键字: Vipadenant | CEB4520 | BIIB 014 | BIIB014 | inhibit | CEB 4520 | Adenosine Receptor | Inhibitor | P1 receptor

相关产品: Kira8 Hydrochloride | N6-(2-Phenylethyl)adenosine | Aminophylline | A3AR agonist 2 | Fostamatinib | KFM19 | GR79236 | Preladenant | Derenofylline | Theophylline monohydrate

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Human Metabolite Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library

化合物Vipadenant T2373信息由TargetMol中国为您提供，如您想了解更多关于化合物Vipadenant T2373报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途