1. GPCR/G Protein Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. ACT-335827

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。

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ACT-335827 Chemical Structure

ACT-335827 Chemical Structure

CAS No. : 1354039-86-3

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查看 Orexin Receptor (OX Receptor) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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 Kb values of 41 nM and 560 nM, the IC50 values of 120 nM and 2300 nM, respectively in CHO cells[1].

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

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].

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

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
性状

固体

颜色

Off-white to light yellow

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
纯度 & 产品资料

纯度: ≥98.0%

参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
ACT-335827
目录号:
HY-108683
需求量: