Aripiprazole (Synonyms: 阿立哌唑; OPC-14597)

目录号: HY-14546 纯度: 99.95%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Aripiprazole (OPC-14597) 是一种非典型抗精神病药，是一种有效、高亲和力的多巴胺 D2 受体部分激动剂。Aripiprazole 在 5-HT2B 和 5-HT2A 受体上是一种反向激动剂，并在 5-HT1A、5-HT2C、D3 和 D4 受体上显示部分激动剂作用。Aripiprazole 可用于精神分裂症和 COVID19 的研究。

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Aripiprazole Chemical Structure

CAS No. : 129722-12-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥660	In-stock
100 mg	￥533	In-stock
200 mg	￥740	In-stock
500 mg		询价
1 g		询价

or 大包装询价

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Customer Review

Other Forms of Aripiprazole:

Aripiprazole-d₈ In-stock
Aripiprazole (1,1,2,2,3,3,4,4-d₈) In-stock
Aripiprazole monohydrate 询价
Aripiprazole (Standard) 询价

MCE 顾客使用本产品发表的 8 篇科研文献

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5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

生物活性
纯度 & 产品资料
参考文献

生物活性

Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19^[1]^[2]^[3]^[4].

IC₅₀ & Target

5-HT_1A Receptor

4.2 nM (Ki)

5-HT_2A Receptor

5-HT_2B Receptor

5-HT_2C Receptor

D₂ Receptor

D₃ Receptor

D₄ Receptor

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	IC₅₀	7.6 nM Compound: 1a	Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay	[PMID: 23237836]
HEK293	IC₅₀	> 100 μM Compound: 1	Cytotoxicity against HEK293 cells measured after 24 hrs by MTT assay Cytotoxicity against HEK293 cells measured after 24 hrs by MTT assay	[PMID: 35176563]
HEK293	EC₅₀	> 5 μM Compound: Aripiprazole	Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay	[PMID: 28300398]
HEK293	EC₅₀	> 5 μM Compound: Aripiprazole	Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay	[PMID: 28300398]
HEK293	EC₅₀	> 5 μM Compound: Aripiprazole	Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay	[PMID: 28300398]
HEK293	EC₅₀	> 5 μM Compound: Aripiprazole	Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay	[PMID: 28300398]
HEK293	IC₅₀	> 500 μM Compound: aripiprazole	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	11 nM Compound: 2a, Aripiprazole	Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay	[PMID: 24831693]
HEK293	IC₅₀	130 μM Compound: aripiprazole	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	EC₅₀	160 nM Compound: 2a, Aripiprazole	Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay	[PMID: 24831693]
HEK293	EC₅₀	20 nM Compound: 2a, Aripiprazole	Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay	[PMID: 24831693]
HEK293	IC₅₀	239 μM Compound: aripiprazole	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK-293T	EC₅₀	1 nM Compound: 1	Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay	[PMID: 22845053]
HEK-293T	EC₅₀	1100 nM Compound: Aripiprazole	Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay	[PMID: 28489379]
HEK-293T	EC₅₀	130 nM Compound: Aripiprazole	Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding	[PMID: 28489379]
HEK-293T	EC₅₀	160 nM Compound: 1a	Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing Galphai2 incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	[PMID: 28248104]
HEK-293T	EC₅₀	20 nM Compound: 1a	Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	[PMID: 28248104]
HEK-293T	EC₅₀	39 nM Compound: 1a	Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay Agonist activity at human Dopamine D2S receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay	[PMID: 28248104]
HEK-293T	EC₅₀	740 nM Compound: Aripiprazole	Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay	[PMID: 28489379]

体外研究
(In Vitro)

Aripiprazole potently activates D2 receptor-mediated inhibition of cAMP accumulation^[1].
Aripiprazole shows a greater anti-inflammatory effect on TNF-α, IL-13, IL-17α and fractalkine^[3].

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

体内研究
(In Vivo)

Aripiprazole (0-3 mg/kg, IP, daily) shows some anxiolytic properties^[4].

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

Animal Model:	WAG/Rij rats (N = 6 per dose, 6 months, administration of a mixture of tiletamine/zolazepam)^[4]
Dosage:	0, 0.3, 1, 3 mg/kg
Administration:	IP, 1 mL/kg, every day at 5 p.m. until the end of the experiments
Result:	Showed some anxiolytic properties with the 1 mg/kg dose being the most active.

Clinical Trial

分子量

448.39

Formula

C₂₃H₂₇Cl₂N₃O₂

CAS 号

129722-12-9

性状

固体

颜色

White to off-white

中文名称

阿立哌唑

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (223.02 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

DMF 中的溶解度 : 50 mg/mL (111.51 mM; 超声助溶)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2302 mL	11.1510 mL	22.3020 mL
5 mM	0.4460 mL	2.2302 mL	4.4604 mL
10 mM	0.2230 mL	1.1151 mL	2.2302 mL

查看完整储备液配制表

* 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 (protect from light)。-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。

摩尔计算器
稀释计算器

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

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)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.58 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.58 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案三

请依序添加每种溶剂： 10% DMF 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.58 mM); 悬浊液; 超声助溶
方案四

请依序添加每种溶剂： 10% DMF 90% Corn Oil
Solubility: 2.5 mg/mL (5.58 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.95%

选择批次：

Data Sheet (628 KB) SDS (394 KB)

COA (195 KB) HNMR (271 KB) LCMS (92 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Burris KD, et al. Aripiprazole, a novel antipsychotic, is a high-affinity partial agonist at human dopamine D2 receptors. J Pharmacol Exp Ther. 2002 Jul;302(1):381-9. [Content Brief]

[2]. Davies MA, et al. Aripiprazole: a novel atypical antipsychotic drug with a uniquely robust pharmacology. CNS Drug Rev. 2004 Winter;10(4):317-36. [Content Brief]

[3]. Crespo-Facorro B, et al. Aripiprazole as a Candidate Treatment of COVID-19 Identified Through Genomic Analysis. Front Pharmacol. 2021 Mar 2;12:646701. [Content Brief]

[4]. Russo E, et al. Ameliorating effects of aripiprazole on cognitive functions and depressive-like behavior in a genetic rat model of absence epilepsy and mild-depression comorbidity. Neuropharmacology. 2013 Jan;64:371-9. [Content Brief]

[5]. Stip E, et al. Aripiprazole in schizophrenia and schizoaffective disorder: A review. Clin Ther. 2010;32 Suppl 1:S3-20. [Content Brief]

Aripiprazole 相关分类

Neurological Disease Inflammation/Immunology Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMF / DMSO	1 mM	2.2302 mL	11.1510 mL	22.3020 mL	55.7550 mL
	5 mM	0.4460 mL	2.2302 mL	4.4604 mL	11.1510 mL
	10 mM	0.2230 mL	1.1151 mL	2.2302 mL	5.5755 mL
	15 mM	0.1487 mL	0.7434 mL	1.4868 mL	3.7170 mL
	20 mM	0.1115 mL	0.5576 mL	1.1151 mL	2.7878 mL
	25 mM	0.0892 mL	0.4460 mL	0.8921 mL	2.2302 mL
	30 mM	0.0743 mL	0.3717 mL	0.7434 mL	1.8585 mL
	40 mM	0.0558 mL	0.2788 mL	0.5576 mL	1.3939 mL
	50 mM	0.0446 mL	0.2230 mL	0.4460 mL	1.1151 mL
	60 mM	0.0372 mL	0.1859 mL	0.3717 mL	0.9293 mL
	80 mM	0.0279 mL	0.1394 mL	0.2788 mL	0.6969 mL
	100 mM	0.0223 mL	0.1115 mL	0.2230 mL	0.5576 mL

Help & FAQs

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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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Aripiprazole (Synonyms: 阿立哌唑; OPC-14597)

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Other Forms of Aripiprazole:

MCE 顾客使用本产品发表的 8 篇科研文献

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•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 5-HT Receptor 亚型特异性产品:

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纯度 & 产品资料

参考文献

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Aripiprazole (Synonyms: 阿立哌唑; OPC-14597)

Customer Review

Other Forms of Aripiprazole:

Aripiprazole 相关抗体

MCE 顾客使用本产品发表的 8 篇科研文献

Aripiprazole 相关产品

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查看 5-HT Receptor 亚型特异性产品:

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生物活性

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参考文献

Aripiprazole 相关抗体:

摩尔计算器

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完整储备液配制表

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