ACT-462206|cas:1361321-96-1|西域试剂

ACT-462206,99.60%

产品编号：Bellancom-101834| CAS NO：1361321-96-1| 分子式：C₂₀H₂₄N₂O₄S| 分子量：388.48

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-101834	￥1500.00	杭州北京（现货）
Bellancom-101834	￥2500.00	杭州北京（现货）
Bellancom-101834	￥5500.00	杭州北京（现货）
Bellancom-101834	￥8500.00	杭州北京（现货）
Bellancom-101834	￥13500.00	杭州北京（现货）

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ACT-462206

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 dual Orexin 1/Orexin 2 receptor antagonist with IC₅₀s 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.

体外研究

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).
ACT-462206 shows binding affinity with K_bs of 17 nM (hOX1), 2.4 nM (hOX2), 28 nM (rOX1), 9.9 nM (rOX2), 27 nM (dOX1), 4.2 nM (dOX2), respectively.
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.
ACT-462206 inhibits CYP450 3A4T and 3A4M with IC₅₀s of 15 μM and 29 μM, respectively.

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

体内研究

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.
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.
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.
Pharmacokinetics in different species

	Route	Dose (mg/kg)	AUC (ng•h/mL)	CL (mL/min/kg)	V_ss (L/kg)	t_1/2 (h)	c_max (ng/mL)	t_max (h)	F_1/2 (%)
rat	i.v.	1	586	29	1.8	1.9	/	/	/
	p.o.	10	2310	/	/	/	1600	0.5	39
dog	i.v.	1	1490	11	1.4	1.7	/	/	/
	p.o.	3	2750	/	/	/	426	0.5	52

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

Animal Model:	Male Wistar rats
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.

体内研究

	Route	Dose (mg/kg)	AUC (ng•h/mL)	CL (mL/min/kg)	V_ss (L/kg)	t_1/2 (h)	c_max (ng/mL)	t_max (h)	F_1/2 (%)
rat	i.v.	1	586	29	1.8	1.9	/	/	/
	p.o.	10	2310	/	/	/	1600	0.5	39
dog	i.v.	1	1490	11	1.4	1.7	/	/	/
	p.o.	3	2750	/	/	/	426	0.5	52

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

Animal Model:	Male Wistar rats
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.

性状

Solid

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 mg	5 mg	10 mg

1 mM	2.5741 mL	12.8707 mL	25.7414 mL
5 mM	0.5148 mL	2.5741 mL	5.1483 mL
10 mM	0.2574 mL	1.2871 mL	2.5741 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°C, 6 months; -20°C, 1 month (protect from light)。-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。

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。