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[1]. |
| IC50& Target | TAAR1 0.140 μM (EC50) | 5-HT1AReceptor 2.3 μM (EC50) | 5-HT1BReceptor 15.6 μM (EC50) | 5-HT1DReceptor 0.262 μM (EC50) | 5-HT2AReceptor >10 μM (EC50) | 5-HT2CReceptor 30 μM (EC50) | 5-HT7Receptor 6.7 μM (EC50) |
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体外研究
(In Vitro) | SEP-856 (10 μM) shows >50% inhibition of specific binding at α2A, α2B, D2, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7receptors[1].
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体内研究
(In Vivo) | SEP-856 (0.3, 1 and 10 mg/kg, i.p.) is CNS active and exhibits a behavioral signature similar to known antipsychotic drugs[1].
SEP-856 (0.3, 1 and 10 mg/kg, orally once) significantly reduces PCP-induced hyperactivity[1].
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[1].
| Animal Model: | Acute treatment with phencyclidine (PCP), which induces robust hyperactivity in rodents[1]. | | 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[1]. | | 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.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 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 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-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： 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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。 *以上所有助溶剂都可在本网站选购。
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