SEP-363856 hydrochloride - CAS:1310422-41-3

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SEP-363856 hydrochloride (Synonyms:SEP-856 hydrochloride)

目录号 : KM10564 CAS No. : 1310422-41-3

Data Sheet 产品使用指南

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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock

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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.

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.

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.

分子式

C₉H₁₄ClNOs

分子量

219.73

CAS号

1310422-41-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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。-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: ≥ 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。
2.

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。
3.

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。