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Bromocriptine Mesylate Dopamine Receptor agonist

Name: Bromocriptine Mesylate
Brand: Selleck Chemicals
SKU: S4309
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4309

Bromocriptine mesylate is a dopamine receptor agonist with a Ki of 12.2 nM for D3 receptor and D2 receptor and a Ki of 1659 nM, 59.7 nM, 1691 nM for D1 receptor, D4 receptor, and D5 receptor, respectively. Bromocriptine mesylate is used in the treatment of Parkinson's disease, hyperprolactinemia-associated dysfunctions, and acromegaly.

Chemical Structure

Molecular Weight: 750.7

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Quality Control

Batch: Purity: 99.95%

99.95

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 SCH-23390 hydrochloride Domperidone SKF38393 HCl Sulpiride Azaperone C-DIM12

Solubility

In vitro
Batch:

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.
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.	5.000mg/ml (6.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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.	0.800mg/ml (1.07mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 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.
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.

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

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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

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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	750.7	Formula	C₃₂H₄₀BrN₅O₅.CH₄O₃S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	22260-51-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)CC1N2C(=O)C(NC(=O)C3CN(C)C4CC5=C(Br)[NH]C6=C5C(=CC=C6)C4=C3)(OC2(O)C7CCCN7C1=O)C(C)C.C[S](O)(=O)=O

Mechanism of Action

Targets/IC₅₀/Ki	D2 receptor 12.2 nM(Ki) D3 receptor 12.2 nM(Ki) D4 receptor 59.7 nM(Ki) D1 receptor 1659 nM(Ki) D5 receptor 1691 nM(Ki)
In vitro	Bromocriptine dose-dependently reduces the number of OH radicals. Bromocriptine has a strong scavenging effect on the 5,5-dimethyl-1-pyrroline-N-oxide hydroxide signal produced from Fenton's reaction. Bromocriptine also attenuates the stable free radical diphenyl-p-picrylhydrazyl signal.
In vivo	Bromocriptine (5 mg/kg, i.p., 7 days) completely protects against the decrease in mouse striatal dopamine and its metabolites induced by intraventricular injection of 6-hydroxydopamine after intraperitoneal administration of desipramine. Bromocriptine (2.5 mg/kg, i.p., daily for 3 days) significantly reduces autooxidation of brain homogenates collected from rats. Bromocriptine (12.5 mg/kg) produces mild dyskinesia over the course of the study that is significantly less severe than in the L-dopa-treated group in the MPTP-treated marmoset. Bromocriptine, has a lesser tendency than L-dopa to produce dyskinesia while similarly improving motor performance in drug-naive MPTP-treated marmosets. Bromocriptine (10 μM and 10 mg/kg i.p.) blocks .OH formation caused by MPTP in vitro (20 μM) and in vivo (30 mg/kg i.p.) in mice. Bromocriptine reduces an MPTP-induced increase in the activity of catalase and superoxide dismutase in substantia nigra on the seventh day. Bromocriptine blocks MPTP-induced behavioral dysfunction as well as glutathione and dopamine depletion, indicating its potent neuroprotective action.
References	[1] https://pubmed.ncbi.nlm.nih.gov/7820619/ [2] https://pubmed.ncbi.nlm.nih.gov/8113789/ [3] https://pubmed.ncbi.nlm.nih.gov/9539335/ [4] https://pubmed.ncbi.nlm.nih.gov/9657530/ [5] https://pubmed.ncbi.nlm.nih.gov/16982285/

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