| CAS NO: | 1354039-86-3 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1354039-86-3 |
| 化学名 | (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 |
| 分子式 | C31H38N2O5 |
| 分子量 | 518.64 |
| 溶解度 | <51.86mg/ml in DMSO;<51.86mg/ml in ethanol |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | ACT 335827 is a potent and selective antagonist of OXR-1 with IC50 values of 120 and 2300 nM for OXR-1 and OXR-2, respectively [1]. Orexin receptor 1 (OXR-1) is a G-protein coupled receptor for neuropeptide orexin-A and regulates feeding behaviour. OXR-1 is expressed in the hypothalamus. ACT 335827 is a potent and selective OXR-1 antagonist with Kb values of 41 and 560 nM for OXR-1 and OXR-2, respectively [1]. In the fear-potentiated startle rats, ACT-335827 (300 mg/kg) inhibited fear-induced startle reactions. Also, ACT-335827 (300 mg/kg) significantly reduced stress-induced tachycardia and hyperthermia. In the rat polydipsia model, ACT-335827 (300 mg/kg) inhibited compulsive drinking behavior [1]. In rats exposed to novelty stress, ACT-335827 (100 mg/kg) reduced the tachycardic and pressor by 48% and 32%, respectively [2]. In a diet-induced obesity(DIO) rat model, ACT-335827 increased the level of high-density lipoprotein and water intake. Also, it slightly increased body weight, which suggested that inhibition of OXR-1 had minimal impact in this model [3]. References: |
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