| CAS NO: | 1354039-86-3 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | Off-white solid |
| Storage | Store at -20°C |
| M.Wt | 518.64 |
| Cas No. | 1354039-86-3 |
| Formula | C31H38N2O5 |
| Solubility | <51.86mg/ml in DMSO;<51.86mg/ml in ethanol |
| Chemical Name | (R,Z)-2-((S)-1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-isopropyl-2-phenylacetimidic acid |
| Canonical SMILES | CC(/N=C(O)/[C@@](N1CCC2=CC(OC)=C(OC)C=C2[C@]1([H])CC3=CC(OC)=C(OC)C=C3)([H])C4=CC=CC=C4)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
ACT 335827是OXR-1的有效选择性拮抗剂,对OXR-1和OXR-2的IC50值分别为120和2300 nM[1].
食欲素受体1(OR-1)是神经肽食欲素A的G蛋白偶联受体,调节摄食行为.OXR-1在下丘脑中表达.
ACT 335827是OXR-1的强效选择性拮抗剂,对OXR-1和OXR-2的Kb值分别为41和560 nM[1].
在恐惧增强惊吓老鼠中,300 mg/kg的ACT-335827抑制恐惧引起的惊吓反应.此外,300 mg/kg的ACT-335827显著减少应激诱导的心动过速和发热.在大鼠烦渴模型中,300 mg/kg的ACT-335827抑制强迫饮酒行为[1].在暴露于新颖性应激的大鼠中,100 mg/kg的ACT-335827分别减少48％和32％的心动过速和升压[2].在饮食诱导的肥胖(DIO)大鼠模型中,ACT-335827增加高密度脂蛋白的水平和水的摄入量.此外,ACT-335827略微增加体重,表明OXR-1抑制在该模型中具有最小的影响[3].
参考文献：
[1]. Steiner MA, Gatfield J, Brisbare-Roch C, et al. Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist. ChemMedChem, 2013, 8(6): 898-903.
[2]. Beig MI, Dampney BW, Carrive P. Both Ox1r and Ox2r orexin receptors contribute to the cardiovascular and locomotor components of the novelty stress response in the rat. Neuropharmacology, 2015, 89: 146-156.
[3]. Steiner MA, Sciarretta C, Pasquali A, et al. The selective orexin receptor 1 antagonist ACT-335827 in a rat model of diet-induced obesity associated with metabolic syndrome. Front Pharmacol, 2013, 4: 165.
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