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Submit ReviewBromocriptine mesylate is a selective D3 and D2 dopamine receptor agonist (Ki values are ~ 5 nM and ~ 8 nM respectively). Activates both isoforms of D2 receptor (EC50 values are 0.10-0.12 nM and 4.4 nM for D2L and D2S receptors, respectively. Bromocriptine shows anti-Aβ effects that are increased in combination with Cromolyn (Cat. No. 6424) and Topiramate (Cat. No. 3620). Also lowers glucose and increases insulin sensitivity in vivo.
Bromocriptine mesylate is also offered as part of the Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 750.7 |
公式 | C32H40BrN5O5.CH3SO3H |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 22260-51-1 |
PubChem ID | 31100 |
InChI Key | NOJMTMIRQRDZMT-GSPXQYRGSA-N |
Smiles | [H][C@]4([C@@](N[C@]([C@H](C)C)5C(N([C@@]([H])(CC(C)C)C(N(CCC7)[C@@]76[H])=O)[C@@]6(O)O5)=O)=O)CN([C@](C3=C4)([H])CC1=C(Br)NC2=C1C3=CC=C2)C.CS(=O)(O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 75.07 | 100 |
以下数据基于产品分子量 750.7。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.33 mL | 6.66 mL | 13.32 mL |
5 mM | 0.27 mL | 1.33 mL | 2.66 mL |
10 mM | 0.13 mL | 0.67 mL | 1.33 mL |
50 mM | 0.03 mL | 0.13 mL | 0.27 mL |
参考文献是支持产品生物活性的出版物。
Aubner et al (1990) Bromocriptine produces decreases in cocaine self-administration in the rat. Neuropsychopharmacology 3 101 PMID: 2317262
Lieberman and Goldstein (1985) Bromocriptine in Parkinson disease. Pharmacol.Rev. 37 217 PMID: 3901046
Seeman and Van Tol (1994) DA receptor pharmacology. TiPS 15 264 PMID: 7940991
Traub et al (1985) The effects of chronic bromocri. treatment on behaviour and DA receptor binding in the rat striatum. Eur.J.Pharmacol. 118 147 PMID: 3936723
Kondo et al (2017) iPSC-based compound screening and in vitro trials identify a synergistic anti-amyloid β combination for Alzheimer's disease. Cell Rep. 21 2304 PMID: 29166618
Tavares et al (2021) Dopamine D2 receptor agonist, bromocriptine, remodels adipose tissue dopaminergic signalling and upregulates catabolic pathways, improving metabolic profile in type 2 diabetes. Mol.Metab. 51 101241 PMID: 33933677
If you know of a relevant reference for Bromocriptine mesylate, please let us know.
关键词: Bromocriptine mesylate, Bromocriptine mesylate supplier, Selective, D2-like, agonists, Dopamine, Non-Selective, Receptors, D3, D4, dopaminergic, insulin, glucose, Ab, Abeta, amyloid, alzheimers, antidiabetic, Non-selective, Amyloid, Beta, Peptides, 0427, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Bromocriptine mesylate 的部分引用包括:
Liberante et al (2016) Identification and validation of the DA agonist bromocri. as a novel therapy for high-risk myelodysplastic syndromes and secondary acute myeloid leukemia. Oncotarget 7 6609 PMID: 26735888
Jia et al (2013) Age-dependent regulation of synaptic connections by DA D2 receptors. Nat Neurosci 16 1627 PMID: 24121738
Pedersen et al (2021) A novel luminescence-based-β-arrestin recruitment assay for unmodified receptors. J Biol Chem 296 100503 PMID: 33684444
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.