Seltorexant hydrochloride JNJ-42847922 hydrochloride|cas:1293284-49-7|西域试剂

Seltorexant hydrochloride JNJ-42847922 hydrochloride,99.90%

产品编号：Bellancom-109012A| CAS NO：1293284-49-7| 分子式：C₂₁H₂₃ClFN₇O| 分子量：443.91

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货号	价格	库存与货期
Bellancom-109012A	￥1100.00	杭州北京（现货）
Bellancom-109012A	￥1650.00	杭州北京（现货）
Bellancom-109012A	￥4550.00	杭州北京（现货）
Bellancom-109012A	￥7200.00	杭州北京（现货）
Bellancom-109012A	￥14500.00	杭州北京（现货）

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Seltorexant hydrochloride JNJ-42847922 hydrochloride

产品介绍

Seltorexant hydrochloride (JNJ-42847922 hydrochloride) 是一种具有口服活性的，高亲和性以及选择性的 OX2R 拮抗剂 (人和大鼠中的 OX2R 的pK_i 值分别为 8.0 和 8.1)。Seltorexant hydrochloride 穿过血脑屏障，迅速占据大鼠大脑中的 OX2R 结合位点。

生物活性

Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pK_i values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.

体外研究

体内研究

Seltorexant hydrochloride (JNJ-42847922 hydrochloride) (3-30 mg/kg; p.o.) dose-dependently induces and prolongs sleep in male Sprague-Dawley rats.
The sleep-promoting effects of Seltorexant hydrochloride (30 mg/kg; p.o.; per day for 7 days) are maintained upon 7-day repeated dosing in rats.

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

Animal Model:	Male Sprague-Dawley rats (350-450 g)
Dosage:	30 mg/kg
Administration:	p.o.; per day for 7 days
Result:	The reduced sleep onset (non–rapid eye movement (NREM) latency) and the increased NREM sleep duration were maintained upon 7-day repeated dosing with JNJ-42847922. The prolongation of NREM sleep time was due to a significant increase in NREM bout duration throughout the treatment period assessed on D1 and D7. Rapid eye movement (REM) sleep was only marginally affected on D4 of treatment, resulting in a small but significant reduction in REM sleep latency and an increase in REM sleep duration.

体内研究

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

Animal Model:	Male Sprague-Dawley rats (350-450 g)
Dosage:	30 mg/kg
Administration:	p.o.; per day for 7 days
Result:	The reduced sleep onset (non–rapid eye movement (NREM) latency) and the increased NREM sleep duration were maintained upon 7-day repeated dosing with JNJ-42847922. The prolongation of NREM sleep time was due to a significant increase in NREM bout duration throughout the treatment period assessed on D1 and D7. Rapid eye movement (REM) sleep was only marginally affected on D4 of treatment, resulting in a small but significant reduction in REM sleep latency and an increase in REM sleep duration.

性状

Solid

溶解性数据

In Vitro:

H₂O : 100 mg/mL (225.27 mM; Need ultrasonic)

DMSO : 83.33 mg/mL (187.72 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2527 mL	11.2635 mL	22.5271 mL
5 mM	0.4505 mL	2.2527 mL	4.5054 mL
10 mM	0.2253 mL	1.1264 mL	2.2527 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 (sealed storage, away from moisture)。-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: ≥ 2.08 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.69 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。