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  2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. Aripiprazole

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

目錄號: HY-14546 純度: 99.95%
COA 產(chǎn)品使用指南 技術(shù)支持

Aripiprazole (OPC-14597) 是一種非典型抗精神病藥，是一種有效、高親和力的多巴胺 D2 受體部分激動劑。Aripiprazole 在 5-HT2B 和 5-HT2A 受體上是一種反向激動劑，并在 5-HT1A、5-HT2C、D3 和 D4 受體上顯示部分激動劑作用。Aripiprazole 可用于精神分裂癥和 COVID19 的研究。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Aripiprazole Chemical Structure

Aripiprazole Chemical Structure

CAS No. : 129722-12-9

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥660
In-stock
100 mg ￥533
In-stock
200 mg ￥740
In-stock
500 mg   詢價  
1 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Aripiprazole:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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-HT1A Receptor

4.2 nM (Ki)

5-HT2A Receptor

 

5-HT2B Receptor

 

5-HT2C Receptor

 

D2 Receptor

 

D3 Receptor

 

D4 Receptor

 

細胞效力
(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]
體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

White to off-white

中文名稱

阿立哌唑
運輸條件

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

4°C, protect from light

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

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : ≥ 100 mg/mL (223.02 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

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

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.58 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.58 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

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

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.95%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
Aripiprazole
目錄號：
HY-14546
需求量：