Bromocriptine mesylate

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CAS NO:

22260-51-1

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at RT
M.Wt	750.7
Cas No.	22260-51-1
Formula	C₃₂H₄₀BrN₅O₅·CH₃SO₃H
Solubility	insoluble 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
Canonical SMILES	BrC(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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

试验操作

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.