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ACT-335827 是一种可口服的、脑渗透性 orexin 1 型 (orexin type 1) 受体选择性拮抗剂。ACT-33582 作用于 OXR1 和 OXR2 的 IC50值分别是 6 nM 和 417 nM。ACT-33582 可用于神经系统疾病的相关研究。
ACT-335827 是一种可口服的、脑渗透性 orexin 1 型 (orexin type 1) 受体选择性拮抗剂。ACT-33582 作用于 OXR1 和 OXR2 的 IC50值分别是 6 nM 和 417 nM。ACT-33582 可用于神经系统疾病的相关研究。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥ 7,980 | 35日内发货 | |
50 mg | ¥ 32,200 | 35日内发货 |
产品描述 | ACT-335827 is an orally available, brain-penetrant orexin type 1 receptor selective antagonist. ACT-33582 acts on OXR1 and OXR2 with IC 50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders [1]. |
体外活性 | ACT-335827 (0-10 μM, 2 h) is active on OXR-1 and OXR-2 with the Kb values of 41 nM and 560 nM, the IC 50 values of 120 nM and 2300 nM, respectively in CHO cells [1]. |
体内活性 | ACT-335827 (oral gavage, 30-100 mg/kg, once) can reduce the fear-induced startle response without affecting motor or cognitive function in rats [1]. ACT-335827 (oral administration, 300 mg/kg, everyday, 4 weeks) has less effect on metabolic syndrome (MetS), such as diet-induced obesity (DIO) in male Wistar rats [2]. Animal Model: Rats [1] Dosage: 30, 100 or 300 mg/kg Administration: Oral gavage; once Result: Reduced fear-induced startle response at 300 mg/kg. Decreased stress-induced elevated body temperature at 300 mg/kg and accelerated heat rate at 100 or 300 mg/kg but no effect on locomotion and blood pressure. Animal Model: Male Wistar rats weighing160-180g [2] Dosage: 300 mg/kg Administration: Oral administration; everyday; 4 weeks Result: Reduced preference for high fat/sweet diets but no effect on absolute energy intake. Increased water intake and HDL relative to total cholesterol. Resulted in a 4% weight gain compared to the control group. |
分子量 | 518.64 |
分子式 | C31H38N2O5 |
CAS No. | 1354039-86-3 |
密度 | 1.144 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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