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编 号:F134649
分子式:C31H38N2O5
分子量:518.64
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1mg
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5mg
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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.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.
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