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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1 mg ¥2920
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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
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 51.864 mg/mL (100.00 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

Ethanol 中的溶解度 : 51.864 mg/mL (100.00 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9281 mL 9.6406 mL 19.2812 mL
5 mM 0.3856 mL 1.9281 mL 3.8562 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥98.0%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 1.9281 mL 9.6406 mL 19.2812 mL 48.2030 mL
5 mM 0.3856 mL 1.9281 mL 3.8562 mL 9.6406 mL
10 mM 0.1928 mL 0.9641 mL 1.9281 mL 4.8203 mL
15 mM 0.1285 mL 0.6427 mL 1.2854 mL 3.2135 mL
20 mM 0.0964 mL 0.4820 mL 0.9641 mL 2.4101 mL
25 mM 0.0771 mL 0.3856 mL 0.7712 mL 1.9281 mL
30 mM 0.0643 mL 0.3214 mL 0.6427 mL 1.6068 mL
40 mM 0.0482 mL 0.2410 mL 0.4820 mL 1.2051 mL
50 mM 0.0386 mL 0.1928 mL 0.3856 mL 0.9641 mL
60 mM 0.0321 mL 0.1607 mL 0.3214 mL 0.8034 mL
80 mM 0.0241 mL 0.1205 mL 0.2410 mL 0.6025 mL
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: