ACT-335827

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ACT-335827

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1354039-86-3

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-penetrantorexin type 1receptor antagonist. ACT-33582 acts on OXR1 and OXR2 withIC₅₀values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders^[1].

IC₅₀& Target^[1]

OX1

6 nM (IC₅₀)

OX2

417 nM (IC₅₀)

体外研究
(In Vitro)

ACT-335827 (0-10 μM, 2 h) acts on OXR-1 and OXR-2 with the K_bvalues of 41 nM and 560 nM, the IC₅₀values of 120 nM and 2300 nM, respectively in CHO cells^[1].

体内研究
(In Vivo)

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^[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

Formula

C₃₁H₃₈N₂O₅

CAS 号

1354039-86-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.