SEP-363856 hydrochloride SEP-856 hydrochloride|cas:1310422-41-3|西域试剂

SEP-363856 hydrochloride SEP-856 hydrochloride,99.57%

产品编号：Bellancom-136109| CAS NO：1310422-41-3| 分子式：C₉H₁₄ClNOS| 分子量：219.73

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-136109	￥3000.00	杭州北京（现货）
Bellancom-136109	￥5000.00	杭州北京（现货）
Bellancom-136109	￥12500.00	杭州北京（现货）
Bellancom-136109	￥0.00	杭州北京（现货）

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SEP-363856 hydrochloride SEP-856 hydrochloride

产品介绍

SEP-363856 (SEP-856) hydrochloride 是具有口服活性的、中枢神经系统活性的抗精神病活性化合物，具有研究精神分裂症的潜力。

生物活性

SEP-363856 hydrochloride (SEP-856 hydrochloride), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride (SEP-856 hydrochloride) has the potential for the study of schizophrenia.

体外研究

SEP-856 (10 μM) shows >50% inhibition of specific binding at α_2A, α_2B, D₂, 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_2A, 5-HT_2B, 5-HT_2C, and 5-HT₇ receptors.

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

体内研究

SEP-856 (0.3, 1 and 10 mg/kg, i.p.) is CNS active and exhibits a behavioral signature similar to known antipsychotic drugs.
SEP-856 (0.3, 1 and 10 mg/kg, orally once) significantly reduces PCP-induced hyperactivity.
Oral SEP-856 administration (1, 3 and 10 mg/kg) produces a dosedependent decrease in REM sleep, increase in latency to REM sleep and increase in cumulative wake (W) time.

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

Animal Model:	Acute treatment with phencyclidine (PCP), which induces robust hyperactivity in rodents.
Dosage:	0.3, 1 and 3 mg/kg.
Administration:	Orally once.
Result:	Resulted in a dose-dependent inhibition of PCP-induced hyperactivity responses in C57Bl/6J mice (1-way ANOVA F_{(5, 59)} = 18.96, p < 0.0001; Tukey’s post-hoc test, p < 0.05) with a 50% effective dose (ED₅₀) of approximately 0.3 mg/kg.

Animal Model:	Male Sprague Dawley rats.
Dosage:	1, 2, and 5 mg/kg.
Administration:	I.V. injection. (Pharmacokinetic Analysis).
Result:	Rapidly absorbed with maximum plasma and brain concentrations reached within 0.25 to 0.5 hours in mice and rats and maximum plasma concentrations reached within 6 ± 2.83 hours in monkeys. Penetrated mouse and rat brains after oral administration (10 mg/kg), with average brain-to-plasma AUC ratios of ~3 respectively.

体内研究

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

Animal Model:	Acute treatment with phencyclidine (PCP), which induces robust hyperactivity in rodents.
Dosage:	0.3, 1 and 3 mg/kg.
Administration:	Orally once.
Result:	Resulted in a dose-dependent inhibition of PCP-induced hyperactivity responses in C57Bl/6J mice (1-way ANOVA F_{(5, 59)} = 18.96, p < 0.0001; Tukey’s post-hoc test, p < 0.05) with a 50% effective dose (ED₅₀) of approximately 0.3 mg/kg.

Animal Model:	Male Sprague Dawley rats.
Dosage:	1, 2, and 5 mg/kg.
Administration:	I.V. injection. (Pharmacokinetic Analysis).
Result:	Rapidly absorbed with maximum plasma and brain concentrations reached within 0.25 to 0.5 hours in mice and rats and maximum plasma concentrations reached within 6 ± 2.83 hours in monkeys. Penetrated mouse and rat brains after oral administration (10 mg/kg), with average brain-to-plasma AUC ratios of ~3 respectively.

性状

Solid

溶解性数据

In Vitro:

H₂O : 100 mg/mL (455.10 mM; Need ultrasonic)

DMSO : 62.5 mg/mL (284.44 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.5510 mL	22.7552 mL	45.5104 mL
5 mM	0.9102 mL	4.5510 mL	9.1021 mL
10 mM	0.4551 mL	2.2755 mL	4.5510 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： PBS
Solubility: 100 mg/mL (455.10 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 6.25 mg/mL (28.44 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (28.44 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 6.25 mg/mL (28.44 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (28.44 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 6.25 mg/mL (28.44 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (28.44 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 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。