Name: Cabergoline
Brand: Selleck Chemicals
SKU: S5842
Availability: InStock
Rating: 5 (2 reviews)

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Quality Control

Batch: Purity: 99.82%

99.82

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Dopamine Receptor Inhibitors	MPTP Hydrochloride Trifluoperazine Trifluoperazine 2HCl Penfluridol Sulpiride SCH-23390 hydrochloride Levosulpiride Domperidone SKF38393 HCl Rotundine

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (199.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 90 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.750mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	451.60	Formula	C₂₆H₃₇N₅O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	81409-90-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	FCE-21336			Smiles	CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C

Mechanism of Action

Targets/IC₅₀/Ki	D2 receptor 0.7 nM 5-HT2 1.2 nM 5-HT2B 1.2 nM D3 receptor 1.5 nM D4 receptor 9 nM
In vitro	Cabergoline prevents the oxidative stress-induced cell death of cultured cortical neurons via a D2 receptor-mediated mechanism. This compound suppresses the activation of ERK signaling, which might have a role in the neuroprotection. It significantly represses extracellular glutamate accumulation triggered by oxidative stress, and increases the expression of glutamate transporters including EAAC1, which is known to be involved in the clearance of extracellular glutamate.
In vivo	Cabergoline has a long elimination half-life (63 to 109 h). An in vivo study of neuronal damage induced by intracerebroventricular (icv) injection of 6-OHDA, a neurotoxic compound that selectively damages dopaminergic neurons in male ICR mice, demonstrates that intraperitoneal (ip) administration of this compound for 7 days prevented nigrostriatal region dopaminergic neurons from cell death. It also protects SH-SY5Y neuroblastoma from cell death by oxygen-glucose deprivation even when this chemical is administered after the induction of cell death. This compound increases hippocampal brain-derived neurotrophic factor (BDNF, an important regulator in the synaptic plasticity) and exerts an antidepressant effect in rats.
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4051758/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03965572	Unknown status	Lactation Suppressed\|Cabergoline Adverse Reaction\|Postpartum DVT\|Postpartum Depression	Laniado Hospital	June 7 2019	--
NCT03457389	Recruiting	Pituitary Adenoma\|Prolactinoma\|Pituitary Tumor\|Recurrence Tumor	Seoul National University Hospital	February 22 2018	Not Applicable
NCT01651364	Completed	Cocaine Dependence\|Cocaine Abuse\|Cocaine Addiction\|Substance Abuse	Baylor College of Medicine\|National Institute on Drug Abuse (NIDA)	July 2011	Phase 1
NCT01270711	Completed	Parkinson''s Disease\|Hyperprolactinemia	Pfizer	November 2010	--
NCT01009567	Completed	Ovarian Hyperstimulation Syndrome	Royan Institute	June 2009	Phase 1\|Phase 2
NCT00153972	Completed	Parkinson''s Disease	Technische Universität Dresden\|Pfizer	February 2005	Phase 4

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Cabergoline Dopamine Receptor agonist

Chemical Structure

Molecular Weight: 451.60