A-381393 - Dopamine Receptor Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEA-381393Cat. No.: HY-116941CAS No.: 726174-00-1分式: CHN分量: 320.43作靶点: Dopamine Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 51.67 mg/mL (161

2、.25 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1208 mL 15.6040 mL 31.2081 mL5 mM 0.6242 mL 3.1208 mL 6.2416 mL10 mM 0.3121 mL 1.5604 mL 3.1208 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；

3、澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (8.05 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (8.05 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.58

4、mg/mL (8.05 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 A-381393种有效、选择性、可透过脑屏障的 dopamine D4 receptor 拮抗剂，对 dopamineD4.4，D4.2 和 D4.7 受体的 Ki 值分别为 1.5，1.9 和 1.6 nM，选择性是对 D1，D2，D3，D5 多巴胺受体的2700 多倍。A-381393 对 5-HT2A 的选择性适中，Ki 值为 370 nM 1。IC50 & Target Ki: 1.

5、5 nM (D4.4 receptor), 1.9 nM (D4.2 receptor), 1.6 nM (D4.7 receptor) 1体外研究 A-381393 exhibits weak affinity at 5-HT1A, Sigma 2, Adenoceptor 1A, Adenoceptor 2C, Histamine H1,with Kis of 1365, 8600, 2044, 1912 and 2962 nM, respectively 1.REFERENCES1. Nakane M, et al. 2-4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl-1H benzoimidazole (A-381393), a selective dopamine D4 receptorantagonist. Neuropharmacology. 2005 Jul;49(1):112-21.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-379