Cat. No.: HY-15296

Cabergoline

(Synonyms: FCE-21336)

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Cabergoline is an ergot derived-dopamine D₂-like receptor agonist that has high affinity for D₂, D₃, and 5-HT_2B receptors (K_i=0.7, 1.5, and 1.2, respectively).

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Pureté: 99.86%
CAS No.: 81409-90-7
Formule: C₂₆H₃₇N₅O₂
Masse moléculaire:451.60

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cabergoline Chemical Structure

CAS No.: 81409-90-7

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (13)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cabergoline is an ergot derived-dopamine D₂-like receptor agonist that has high affinity for D₂, D₃, and 5-HT_2B receptors (K_i=0.7, 1.5, and 1.2, respectively).

IC₅₀ & Target

D₃ Receptor

D₂ Receptor

5-HT_2B Receptor

Voir tous les produits spécifiques à Isoform Dopamine Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	13 nM Compound: Cabergoline	Agonist activity at human 5-HT2B receptor transfected in CHO cell assessed as IP1 production incubated for 30 mins measured by HTRF detection method Agonist activity at human 5-HT2B receptor transfected in CHO cell assessed as IP1 production incubated for 30 mins measured by HTRF detection method	[PMID: 23606928]

In Vitro

Cabergoline acts as a potent agonist of D₂, D₃ and 5-HT_2B receptors. Pretreatment with Cabergoline inhibits H₂O₂-induced neuronal cell death in a dose-dependent manner. In the following experiments, 10 μM of Cabergoline is used to investigate its neuroprotective effects. MAP2 staining reveals that Cabergoline significantly suppresses the loss of neurons caused by H₂O₂ incubation. The detection of apoptotic nuclear condensation suggested that Cabergoline prevents apoptotic cell death following H₂O₂ exposure^[1].

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

In Vivo

The most significant reduction in rapid eye movement (REM) sleep bout number occurred during the light phase, in which Cabergoline-injected female handled mice has 67.3% less REM sleep bouts (F_(1,11)=12.892, P=0.004), although the greatest number in reduction of REM sleep bouts occurr during the dark phase (82.3% fewer REM sleep bouts; F_(1,11)=3.667, P=0.082). In male mice, Cabergoline reduces baseline Prolactin (PRL) levels (98.5%; F_(1,6)=13.192, P=0.011) from 5.8±1.3 to 0.08 ng/mL within 2 hours of injection. After a 7-day recovery period, PRL levels return to values that are not different from baseline (5.0±0.60 ng/mL; F_(1,6)=0.715, P=0.43)^[2].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 81409-90-7
Appearance Solid
Masse moléculaire 451.60
Formule C₂₆H₃₇N₅O₂
Color White to off-white
SMILES

C=CCN1[C@@]2([H])[C@@](C[C@H](C1)C(N(CCCN(C)C)C(NCC)=O)=O)([H])C3=CC=CC4=C3C(C2)=CN4
Synonyms

FCE-21336
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

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Journal Impact Factor

Nat Commun

Pyridoxine induces glutathione synthesis via PKM2-mediated Nrf2 transactivation and confers neuroprotection. [Abstract]

2020 Feb 18;11(1):941. PMID: 32071304
J Neuroinflammation

Dopamine signaling governs macrophage-mediated acute lung injury through JAML/IL-10-coupled mitochondrial regulation. [Abstract]

2026 Apr 23. PMID: 42026623
Phytomedicine

Valproic acid promotes transcriptional activation of Drd2 by mediating histone acetylation to inhibit the mTOR-Pttg1 signaling axis and exerts anti-PitNETs activity. [Abstract]

2025 Jun:141:156707. PMID: 40220407
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Int J Mol Med

circOMA1 delivered by exosomes regulates DRD2‑mediated prolactinoma resistance. [Abstract]

2026 Jun;57(6):141. PMID: 41891968
Phytother Res

Hordenine improves Parkinsonian-like motor deficits in mice and nematodes by activating dopamine D2 receptor-mediated signaling. [Abstract]

2023 Aug;37(8):3296-3308. PMID: 36883794
Acta Neuropathol Commun

Cholesterol-activated stress granules reduce the membrane localization of DRD2 and promote prolactinoma dopamine agonists resistance. [Abstract]

2025 Apr 25;13(1):84. PMID: 40281543
Int J Mol Sci

The Activation of p300 Enhances the Sensitivity of Pituitary Adenomas to Dopamine Agonist Treatment by Regulating the Transcription of DRD2. [Abstract]

2024 Nov 21;25(23):12483. PMID: 39684198
Sci Rep

Transcriptomic analysis of the anti-tumor effects of leflunomide in prolactinoma. [Abstract]

2025 Apr 5;15(1):11703. PMID: 40188147
Cancers (Basel)

Alternations of Blood Pressure Following Surgical or Drug Therapy for Prolactinomas. [Abstract]

2024 Feb 9;16(4):726. PMID: 38398117
J Endocrinol Invest

CircOMA1 modulates cabergoline resistance by downregulating ferroptosis in prolactinoma. [Abstract]

2023 Aug;46(8):1573-1587. PMID: 36853491
Exp Cell Res

DEPTOR as a novel prognostic marker inhibits the proliferation via deactivating mTOR signaling pathway in gastric cancer cells. [Abstract]

2023 Apr 11;427(1):113598. PMID: 37054772
IBRO Neurosci Rep

PKD1-mediated phosphorylation at dopamine D2 receptor serine 365 site in dorsal striatum underlies cocaine-induced locomotor hyperactivity. [Abstract]

2025 Jun 19:19:124-132. PMID: 40606639

Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (553.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2143 mL

11.0717 mL

22.1435 mL

5 mM

0.4429 mL

2.2143 mL

4.4287 mL

10 mM

0.2214 mL

1.1072 mL

2.2143 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (4.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

Primary cortical neurons are prepared. Cabergoline (10 µM; except for experiments of dose-dependency) is applied to cortical cells at DIV 6-7. After 24-hour Cabergoline treatment (except for examination of pretreatment time-dependency of Cabergoline), H₂O₂ (50 µM; except for the dose-dependency of H₂O₂) is added. All inhibitors and antagonists, including spiperone, U0126, SB203580, SP600125, AP5, and nifedipine are applied 20 min before Cabergoline or H₂O₂ addition. L-glutamate is added at DIV 7-8 for cell death induction. Cell survival rate is measured by MTT assay. After the indicated treatment with drugs is completed, culture medium is replaced with 200 µL fresh medium containing 40 µl MTT solution (2.5 mg/mL, diluted in PBS) and cells are incubated at 37°C for 1.5-2.5 hours. Then, 200 µL lysis buffer containing isopropyl alcohol is applied to each well and mixed by pipetting. Each sample is moved to a 96-well plate and its absorbance at 570 nm is measured using an iMark Micro plate leader. Cell survival rate is quantitated by absorbance measurement, because MTT (yellow) is deoxidized to formazan (violet) in proportion to mitochondrial activity^[1].

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

Animal Administration^[2]

Mice^[2]
Female and male C57BL/6J mice are used.Cabergoline is dissolved in 100% pharmasolve and then diluted with 20% β-cyclodextrin in water to yield a final concentration of 0.15-0.5 mg/mL Cabergoline. Mice received a 0.3-mg/kg ip injection of Cabergoline or vehicle. All drugs are prepared within 48 hours of experiment and stored at 4°C. Solutions are allowed to reach at room temperature before injection.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Odaka H, et al. Cabergoline, dopamine D2 receptor agonist, prevents neuronal cell death under oxidative stress via reducing excitotoxicity. PLoS One. 2014 Jun 10;9(6):e99271. [Content Brief]

[2]. Jefferson F, et al. A dopamine receptor d2-type agonist attenuates the ability of stress to alter sleep in mice. Endocrinology. 2014 Nov;155(11):4411-21. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2143 mL	11.0717 mL	22.1435 mL	55.3587 mL
	5 mM	0.4429 mL	2.2143 mL	4.4287 mL	11.0717 mL
	10 mM	0.2214 mL	1.1072 mL	2.2143 mL	5.5359 mL
	15 mM	0.1476 mL	0.7381 mL	1.4762 mL	3.6906 mL
	20 mM	0.1107 mL	0.5536 mL	1.1072 mL	2.7679 mL
	25 mM	0.0886 mL	0.4429 mL	0.8857 mL	2.2143 mL
	30 mM	0.0738 mL	0.3691 mL	0.7381 mL	1.8453 mL
	40 mM	0.0554 mL	0.2768 mL	0.5536 mL	1.3840 mL
	50 mM	0.0443 mL	0.2214 mL	0.4429 mL	1.1072 mL
	60 mM	0.0369 mL	0.1845 mL	0.3691 mL	0.9226 mL
	80 mM	0.0277 mL	0.1384 mL	0.2768 mL	0.6920 mL
	100 mM	0.0221 mL	0.1107 mL	0.2214 mL	0.5536 mL

Keywords

Cabergoline

13 Cited Publications

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Cabergoline

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Publications Citing Use of MedChemExpress (MCE) Cabergoline

Voir tous les produits spécifiques à Isoform Dopamine Receptor

Activité biologique

Chemical Information

Publications (13)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Cabergoline Related Classifications

HY-15296 Related Classifications