1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor 5-HT Receptor
  3. Apomorphine

Apomorphine  (Synonyms: (-)-Apomorphine)

目录号: HY-12723 纯度: 98.05%
COA 产品使用指南 技术支持

Apomorphine 是一种有口服活性的 Dopamine receptor 激动剂。Apomorphine 可用于帕金森、双相运动障碍、尿功能障碍、肌张力障碍、呼吸困难、痉挛和打嗝的研究。

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Apomorphine

Apomorphine Chemical Structure

CAS No. : 58-00-4

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规格 价格 是否有货 数量
1 mg ¥1260
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5 mg ¥3150
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Other Forms of Apomorphine:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Apomorphine is an orally active agonist of Dopamine receptor. Apomorphine can be used in study Parkinson, biphasic dyskinesias, urinary dysfunction,,dystonia, dyspnoea, anismus and belching[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Astrocyte EC50
10.19 μM
Compound: 6
Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
[PMID: 17417631]
CHO-K1 EC50
30 nM
Compound: 1
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
Agonist activity at rat D2 dopamine receptor expressed in CHOK1 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counter
[PMID: 21550699]
CHO-K1 IC50
4.2 nM
Compound: Apomorphine
Agonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
Agonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
[PMID: 25557493]
CHO-K1 EC50
53 nM
Compound: 1
Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting
Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting
[PMID: 19454369]
COS-7 IC50
118 nM
Compound: Apomorphine
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
10.1007/s00044-004-0006-x
COS-7 IC50
135 nM
Compound: Apomorphine
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
10.1007/s00044-004-0006-x
COS-7 IC50
24.3 nM
Compound: Apomorphine
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
10.1007/s00044-004-0006-x
COS-7 IC50
27.2 nM
Compound: Apomorphine
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
10.1007/s00044-004-0006-x
COS-7 IC50
29.4 nM
Compound: Apomorphine
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
10.1007/s00044-004-0006-x
COS-7 IC50
69.5 nM
Compound: Apomorphine
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting
10.1007/s00044-004-0006-x
HEK293 EC50
0.4 nM
Compound: Apomorphine
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
0.4 nM
Compound: Apomorphine
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
1.5 nM
Compound: Apomorphine
Agonist activity at ferret D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at ferret D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
1.5 nM
Compound: Apomorphine
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
1.8 nM
Compound: Apomorphine
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
1.8 nM
Compound: Apomorphine
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay
[PMID: 15239663]
HEK293 IC50
20.8 μM
Compound: apomorphine
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
HEK293 EC50
25.7 nM
Compound: 1
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
[PMID: 23727194]
HEK293 EC50
4 nM
Compound: 1
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
Agonist activity at human dopamine D2L receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 15 mins
[PMID: 23727194]
HEK293 EC50
4.3 nM
Compound: Apomorphine
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
4.3 nM
Compound: Apomorphine
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
5.5 nM
Compound: Apomorphine
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
5.5 nM
Compound: Apomorphine
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
5.8 nM
Compound: Apomorphine
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
5.8 nM
Compound: Apomorphine
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay
[PMID: 15239663]
Medulloblastoma cell EC50
0.168 μM
Compound: 6
Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
[PMID: 17417631]
Clinical Trial
分子量

267.32

Formula

C17H17NO2

CAS 号
性状

固体

颜色

Blue to blue-green

中文名称

阿扑吗啡;阿朴吗啡;去水吗啡

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (187.04 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7408 mL 18.7042 mL 37.4083 mL
5 mM 0.7482 mL 3.7408 mL 7.4817 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 (sealed storage, away from moisture)。-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)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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 (9.35 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。

    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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (9.35 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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

g

每只动物的给药体积

μL

动物数量

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 (sealed storage, away from moisture)

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: 99.48%

参考文献

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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7408 mL 18.7042 mL 37.4083 mL 93.5209 mL
5 mM 0.7482 mL 3.7408 mL 7.4817 mL 18.7042 mL
10 mM 0.3741 mL 1.8704 mL 3.7408 mL 9.3521 mL
15 mM 0.2494 mL 1.2469 mL 2.4939 mL 6.2347 mL
20 mM 0.1870 mL 0.9352 mL 1.8704 mL 4.6760 mL
25 mM 0.1496 mL 0.7482 mL 1.4963 mL 3.7408 mL
30 mM 0.1247 mL 0.6235 mL 1.2469 mL 3.1174 mL
40 mM 0.0935 mL 0.4676 mL 0.9352 mL 2.3380 mL
50 mM 0.0748 mL 0.3741 mL 0.7482 mL 1.8704 mL
60 mM 0.0623 mL 0.3117 mL 0.6235 mL 1.5587 mL
80 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1690 mL
100 mM 0.0374 mL 0.1870 mL 0.3741 mL 0.9352 mL
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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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产品名称:
Apomorphine
目录号:
HY-12723
需求量: