1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor Dopamine Receptor Adrenergic Receptor
  3. Brexpiprazole hydrochloride

Brexpiprazole hydrochloride  (Synonyms: OPC-34712 hydrochloride)

目录号: HY-15780A
产品使用指南

Brexpiprazole (OPC-34712) hydrochloride,一种非典型的、具有口服活性的抗精神紊乱剂,是人 5-HT1A 和多巴胺受体(dopamine D2L receptor)的部分激动剂,Ki 分别为 0.12 nM 和 0.3 nM。Brexpiprazole hydrochloride 也是 5-HT2A 受体的拮抗剂,Ki 为 0.47 nM。Brexpiprazole hydrochloride 对人去甲肾上腺素能受体 α1B (Ki=0.17 nM) 和 α2C (Ki=0.59 nM) 也显示出强效拮抗活性。

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Brexpiprazole hydrochloride Chemical Structure

Brexpiprazole hydrochloride Chemical Structure

CAS No. : 913612-38-1

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Brexpiprazole hydrochloride 的其他形式现货产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[1][2].

IC50 & Target

5-HT1A Receptor

0.12 nM (Ki)

5-HT2A Receptor

0.47 nM (Ki)

D2L Receptor

0.3 nM (Ki)

human noradrenergic α1B

0.17 nM (Ki)

human noradrenergic α2C

0.59 nM (Ki)

体外研究
(In Vitro)

Brexpiprazole (0-1.0 μM, 4 days) potentiates NGF-induced neurite outgrowth in a dose-dependent manner in PC12 cells[1].

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

体内研究
(In Vivo)

Brexpiprazole (0-0.1 mg/kg; p.o.; once) improves social recognition deficits in mice[2].

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

Animal Model: Male C57BL/6NCrSlc mice, Dizocilpine (0.1 mg/kg) (HY-15084B) induced social recognition deficits[2]
Dosage: 0.01, 0.03 and 0.1 mg/kg
Administration: Oral administration, once
Result: Significantly ameliorated Dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior.
Clinical Trial
Formula

C25H28ClN3O2S

CAS 号
中文名称

盐酸依匹哌唑

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
  • 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.

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产品名称:
Brexpiprazole hydrochloride
目录号:
HY-15780A
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