Cabergoline (Synonyms: FCE-21336)

Name: Cabergoline
Brand: MedChemExpress
SKU: HY-15296
Rating: 5.0 (6 reviews)

Cat. No.: HY-15296 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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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).

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

Cabergoline Chemical Structure

CAS No. : 81409-90-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 106	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 106	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 558	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Cabergoline:

6 Publications Citing Use of MCE Cabergoline

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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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

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.

Clinical Trial

Molecular Weight

451.60

Formula

C₂₆H₃₇N₅O₂

CAS No.

81409-90-7

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.08 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.
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: ≥ 2.08 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.
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.
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

mg/kg

Animal weight
(per animal)

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).

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: 99.86%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (251 KB) LCMS (86 KB)

Handling Instructions (2659 KB)

References

[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]

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

Complete Stock Solution Preparation Table

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

Cabergoline Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
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.

Keywords:

Cabergoline81409-90-7FCE-21336FCE21336FCE 21336Dopamine ReceptorAutophagyInhibitorinhibitorinhibit

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Cabergoline (Synonyms: FCE-21336)

Customer Review

Other Forms of Cabergoline:

Cabergoline Related Antibodies

6 Publications Citing Use of MCE Cabergoline

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Dopamine Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Cabergoline Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Cabergoline Related Classifications

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