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

Apomorphine  (Synonyms: (-)-Apomorphine)

Cat. No.: HY-12723 Purity: 98.05%
Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

Apomorphine Chemical Structure

Apomorphine Chemical Structure

CAS No. : 58-00-4

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5 mg In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Apomorphine:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

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
Molecular Weight

267.32

Formula

C17H17NO2

CAS No.
Appearance

Solid

Color

Blue to blue-green

SMILES

OC1=CC=C2C(C3=C4C(CCN(C)[C@]4([H])C2)=CC=C3)=C1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (187.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (9.35 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.48%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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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Product Name:
Apomorphine
Cat. No.:
HY-12723
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