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Bromocriptine mesylate

Catalog No.
B6298
A potent, selective D2-like dopamine receptor agonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$72.00
In stock
50mg
$64.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Bromocriptine Mesylate is a potent, selective D2-like dopamine receptor agonist with pKi of 8.05±0.2. Depending on the D2-like dopamine receptor of the target tissue that Bromocriptine Mesylate binds to, it can decrease metabolic processes leading to glucose intolerance and insulin resistance, inhibit the release of pituitary prolactin, and stimulate motor activity in Parkinson's disease. Bromocriptine Mesylate has been approved for treatment of type 2 diabetes, pituitary prolactinomas, acromegaly and Parkinson's disease.?

References:

1.?Gardner B, Strange PG. Agonist action at D2(long) dopamine receptors: ligand binding and functional assays. British Journal of Pharmacology, 1998, 124(5): 978-984.

2.?Ozery M, Wadhwa R. Bromocriptine. [Updated 2021 May 10]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2021 Jan.

3.?Seo EJ, Sugimoto Y, Greten HJ, et al. Repurposing of Bromocriptine for Cancer Therapy. Frontiers in pharmacology, 2018, 9: 1030.

4. Harish Kumar VS, Vinutha MB, Pradeep AN, et al. Bromocriptine, a Dopamine (d2) Receptor Agonist, Used Alone and in Combination with Glipizide in Sub-Therapeutic Doses to Ameliorate Hyperglycaemia.?Journal of clinical and diagnostic research, 2013, 7(9): 1904-1907.

Chemical Properties

Physical AppearanceA solid
StorageStore at RT
M.Wt750.7
Cas No.22260-51-1
FormulaC32H40BrN5O5·CH3SO3H
Solubilityinsoluble in H2O; insoluble in EtOH; ≥20.05 mg/mL in DMSO
Chemical Name(6aR,9R)-5-bromo-N-((2R,5S,10aS,10bS)-10b-hydroxy-5-isobutyl-2-isopropyl-3,6-dioxooctahydro-2H-oxazolo[3,2-a]pyrrolo[2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9-hexahydroindolo[4,3-fg]quinoline-9-carboxamide methanesulfonate
SDFDownload SDF
Canonical SMILESBrC(NC1=CC=CC2=C31)=C3C[C@H](C2=C4)N(C)C[C@@H]4C(N[C@]5(C(C)C)O[C@@]6(N(C5=O)[C@@H](CC(C)C)C(N7[C@H]6CCC7)=O)O)=O.OS(=O)(C)=O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:[3]

Cell lines

Drug-sensitive (CCRF-CEM, HEK293, and MDA-MB-231-pcDNA3) and multidrug-resistant cell lines (CEM/ADR5000, HEK293-ABCB5, and MDA-MB-231-BCRP)

Reaction Conditions

72 h incubation

Applications

Bromocriptine inhibited drug-sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 leukemic cells with IC50 values of 10.13 and 11.78 μM, respectively. Bromocriptine also showed cytotoxic effects toward wild-type or multidrug-resistant ABCB5-transfected HEK293 cell lines, but not sensitive for BCRP-transfected multidrug-resistant MDA-MB-231 breast cancer cells. Bromocriptine inhibited drug-resistant tumor cells with different resistance mechanisms in a hormone-independent manner.
Animal experiment:[4]

Animal models

Alloxan induced diabetic rats

Dosage form

4 mg/kg body wt

Once daily by oral route for 30 consecutive days

Applications

Bromocriptine (4 mg/kg), which was used alone, lowered the blood glucose levels appreciably, whereas the concomitant administration of Bromocriptine (2 mg/kg) and Glipizide (1.25 mg/kg) in sub therapeutic doses produced a much more appreciable reduction. Hence, Bromocriptine may serve as a valuable adjunct to available anti-diabetic medication.

Note

The technical data provided above is for reference only.

References:

1. Gardner B, Strange PG. Agonist action at D2(long) dopamine receptors: ligand binding and functional assays. British Journal of Pharmacology, 1998, 124(5): 978-984.

2. Ozery M, Wadhwa R. Bromocriptine. [Updated 2021 May 10]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2021 Jan.

3. Seo EJ, Sugimoto Y, Greten HJ, et al. Repurposing of Bromocriptine for Cancer Therapy. Frontiers in pharmacology, 2018, 9: 1030.

4. Harish Kumar VS, Vinutha MB, Pradeep AN, et al. Bromocriptine, a Dopamine (d2) Receptor Agonist, Used Alone and in Combination with Glipizide in Sub-Therapeutic Doses to Ameliorate Hyperglycaemia. Journal of clinical and diagnostic research, 2013, 7(9): 1904-1907.

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