ACT-335827,98.0%

产品编号:Bellancom-108683| CAS NO:1354039-86-3| 分子式:C31H38N2O5| 分子量:518.64

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-108683
7300.00 杭州 北京(现货)

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ACT-335827

产品介绍 ACT-335827 是一种选择性的、具有口服活性、可透过血脑屏障的 orexin 1 型 (orexin type 1) 受体拮抗剂。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。
生物活性

ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders.

体外研究

ACT-335827 (0-10 μM, 2 h) acts on OXR-1 and OXR-2 with the Kb values of 41 nM and 560 nM, the IC50 values of 120 nM and 2300 nM, respectively in CHO cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

ACT-335827 (oral gavage, 30-100 mg/kg, once) can reduce the fear-induced startle response with no affecting motor or cognitive function in rats.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats
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
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.
体内研究

ACT-335827 (oral gavage, 30-100 mg/kg, once) can reduce the fear-induced startle response with no affecting motor or cognitive function in rats.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats
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
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.
性状Solid
溶解性数据
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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