2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SEP-363856

SEP-363856  (Synonyms: SEP-856)

目录号: HY-136109A
产品使用指南

摩尔计算器

SEP-363856 (SEP-856) 是具有口服活性的 TAAR1 和 5-HT1A 激动剂、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。

该游离形式化合物不稳定，推荐具有相同生物学活性的稳定盐形式 SEP-363856 hydrochloride。

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SEP-363856 Chemical Structure

SEP-363856 Chemical Structure

CAS No. : 1310426-33-5

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2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

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SEP-363856 的其他形式现货产品:

Customer Review

Other Forms of SEP-363856:

SEP-363856 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SEP-363856 (SEP-856), an orally active TAAR1 and 5-HT1A agonist and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 (SEP-856) has the potential for the study of schizophrenia[1].

IC50 & Target[1]

TAAR1

0.140 μM (EC50)

5-HT1A Receptor

2.3 μM (EC50)

5-HT1B Receptor

15.6 μM (EC50)

5-HT1D Receptor

0.262 μM (EC50)

5-HT2A Receptor

>10 μM (EC50)

5-HT2C Receptor

30 μM (EC50)

5-HT7 Receptor

6.7 μM (EC50)

体外研究
(In Vitro)

SEP-363856 (10 μM) 对 α2A、α2B、D2、5-HT1A、5-HT1B、5-HT1D、5-HT2A、5-HT2B、5-HT2C 和 5-HT7 受体的特异性结合抑制率 >50%[1]。

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

SEP-363856 相关抗体:
体内研究
(In Vivo)

SEP-363856（0.3、1 和 10 mg/kg，腹腔注射）具有中枢神经活性，表现出与已知抗精神病药物类似的行为特征[1]。
SEP-363856（0.3、1 和 10 mg/kg，口服一次）可显著降低 PCP 引起的多动症[1]。
口服 SEP-363856（1、3 和 10 mg/kg）可导致剂量依赖性的 REM 睡眠减少、REM 睡眠潜伏期增加和累积清醒 (W) 时间增加[1]。

MCE 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[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: 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.
Clinical Trial
分子量

183.27

Formula

C9H13NOS
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SEP-363856 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SEP-3638561310426-33-5SEP-856SEP363856SEP 363856SEP856SEP 8565-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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