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ACT-462206
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。
ACT-462206图片
CAS NO:1361321-96-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
ACT-462206 是一种口服有效的双Orexin 1/Orexin 2受体拮抗剂,IC50分别为 60 nM (Orexin 1) 和 11 nM (Orexin 2)。ACT-462206 能穿过血脑屏障,可用于失眠、压力/焦虑相关障碍和成瘾研究。
生物活性

ACT-462206 is an orally active and potent dualOrexin 1/Orexin 2receptor antagonist withIC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research[1].

IC50& Target

OX2

 

OX1

 

体外研究
(In Vitro)

Orexins are released in a Ca2+-sensitive manner at axonal terminals and can then bind to two closely related G-protein-coupled receptors (GPCRs): orexin receptor type 1 (OX1) and orexin receptor type 2 (OX2)[1].
ACT-462206 shows binding affinity with Kbs of 17 nM (hOX1), 2.4 nM (hOX2), 28 nM (rOX1), 9.9 nM (rOX2), 27 nM (dOX1), 4.2 nM (dOX2), respectively[1].
ACT-462206 inhibits Orexin activity with IC50s of 60 nM (hOX1), 11 nM (hOX2), 48 nM (rOX1), 9.6 nM (rOX2), 68 nM (dOX1), 26 nM (dOX2), respectively[1].
ACT-462206 inhibits CYP450 3A4T and 3A4M with IC50s of 15 μM and 29 μM, respectively[1].

体内研究
(In Vivo)

ACT-462206 (compound 24) (100 mg/kg; p.o.; sampling at 3 h) can go cross blood brain barrier, with concentrations are 2267 ng/mL and 1219 ng/g in plasma and brain, respectively in male Wistar rats[1].
ACT-462206 (10-300 mg/kg; p.o.; single dose) shows sleep-promoting effects in male Wistar rats and in male Beagle dogs, with decreasing wakefulness and increasing non-rapid eye movement (non-REM) and REM sleep[1].
ACT-462206 (100, 300 mg/kg; p.o.; single dose) exerts anxiolytic-like effects, decreases the fear-potentiated startle reflexes in response to a sudden loud noise in rats, reduces the socialstress-induced increases of locomotion, body temperature, and heart rate[1].
Pharmacokinetics in different species[1]

RouteDose (mg/kg)AUC (ngoh/mL)CL (mL/min/kg)Vss(L/kg)t1/2(h)cmax(ng/mL)tmax(h)F1/2(%)
rati.v.1586291.81.9///
p.o.102310///16000.539
dogi.v.11490111.41.7///
p.o.32750///4260.552

Animal Model:Male Wistar rats[1]
Dosage:0, 10, 30, 100, 300 mg/kg
Administration:Oral gavage; single dose
Result:Decreased the latency to the first persistent episode of non-REM sleep (60 s) and the first persistent episode of REM sleep (30 s).
Dose-dependently decreased total wake time and behavioral home cage activity (one-way ANOVA; p<0.001), while increasing REM and non-REM sleep times.
Clinical Trial
分子量

388.48

性状

Solid

Formula

C20H24N2O4S

CAS 号

1361321-96-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL(257.41 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5741 mL12.8707 mL25.7414 mL
5 mM0.5148 mL2.5741 mL5.1483 mL
10 mM0.2574 mL1.2871 mL2.5741 mL
*

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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (6.44 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.44 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (6.44 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.44 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。