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Bromocriptine mesylate/甲磺酸溴隐亭 {[allProObj[0].p_purity_real_show]}

货号:A305117 同义名: CB-154; Bromocriptine (mesylate)

Bromocriptine mesylate is a potent dopamine D2/D3 receptoragonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Bromocriptine mesylate/甲磺酸溴隐亭 化学结构 CAS号:22260-51-1
Bromocriptine mesylate/甲磺酸溴隐亭 化学结构
CAS号:22260-51-1
Bromocriptine mesylate/甲磺酸溴隐亭 3D分子结构
CAS号:22260-51-1
Bromocriptine mesylate/甲磺酸溴隐亭 化学结构 CAS号:22260-51-1
Bromocriptine mesylate/甲磺酸溴隐亭 3D分子结构 CAS号:22260-51-1
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Bromocriptine mesylate/甲磺酸溴隐亭 纯度/质量文件 产品仅供科研

货号:A305117 标准纯度: {[allProObj[0].p_purity_real_show]}
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Bromocriptine mesylate/甲磺酸溴隐亭 生物活性

描述 Bromocriptine mesylate (BRC), a dopamine D2 receptor agonist has been shown to confer neuroprotection, sustained motor function and slowed disease progression in mouse models of amyotrophic lateral sclerosis (ALS) Here we report a first in human trial in ALS[3]. Bromocriptine stimulates [35S]-GTPγS binding at D2 dopamine receptor expressed in CHO cells with pEC50 of 8.15±0.05[4]. Bromocriptine is found to inhibit the activity of at least one human cytochrome P450 enzyme. Bromocriptine is a potent inhibitor of CYP3A4 with a calculated IC50 value for the interaction of 1.69 μM[5]. Bromocriptine mesylate (2 mg/kg, i.p.) is administered for 7 days in groups of mice in forced swimming test (FST) and tail suspension test (TST). Bromocriptine group shows significant anti-immobility action as compared to control. When Bromocriptine administered 30 min after the last dose of 7 days MPE treatment and subjected to FST, this dopaminergic agonist produces significant and dose dependent potentiation of anti-immobility action of MPE (200 mg/kg, p.o.) as compared to MPE treatment alone. Bromocriptine treatment group shows a significant reduction of immobility time as compared to control. Bromocriptine administration after 7 days pretreatment with MPE (100 and 200 mg/kg, p.o.) shows significant and dose dependent potentiation of anti-immobility action of MPE as compared to MPE treatment alone[6].

Bromocriptine mesylate/甲磺酸溴隐亭 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00716820 - Completed - -
NCT03492580 - Completed - United States, New Jersey ... 展开 >> Janssen Investigative Site Titusville, New Jersey, United States, 08560 收起 <<
NCT00716820 - Completed - -

Bromocriptine mesylate/甲磺酸溴隐亭 参考文献

[1]Gardner B, Strange PG. Agonist action at D2(long) dopamine receptors: ligand binding and functional assays. Br J Pharmacol. 1998 Jul;124(5):978-84.

[2]Renodon A, Boucher JL, et al. Bromocriptine is a strong inhibitor of brain nitric oxide synthase: possible consequences for the origin of its therapeutic effects. FEBS Lett. 1997 Apr 7;406(1-2):33-6.

[3]Nagata E, Ogino M, Iwamoto K, Kitagawa Y, Iwasaki Y, Yoshii F, Ikeda JE; ALS Consortium Investigators. Bromocriptine Mesylate Attenuates Amyotrophic Lateral Sclerosis: A Phase 2a, Randomized, Double-Blind, Placebo-Controlled Research in Japanese Patients. PLoS One. 2016 Feb 24;11(2):e0149509

[4]Gardner B, Strange PG. Agonist action at D2(long) dopamine receptors: ligand binding and functional assays. Br J Pharmacol. 1998 Jul;124(5):978-84

[5]Wynalda MA, Wienkers LC. Assessment of potential interactions between dopamine receptor agonists and various human cytochrome P450 enzymes using a simple in vitro inhibition screen. Drug Metab Dispos. 1997 Oct;25(10):1211-4

[6]Rana DG, Galani VJ. Dopamine mediated antidepressant effect of Mucuna pruriens seeds in various experimental models of depression. Ayu. 2014 Jan;35(1):90-7

Bromocriptine mesylate/甲磺酸溴隐亭 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.33mL

0.27mL

0.13mL

6.66mL

1.33mL

0.67mL

13.32mL

2.66mL

1.33mL

Bromocriptine mesylate/甲磺酸溴隐亭 技术信息

CAS号22260-51-1
分子式C33H44BrN5O8S
分子量 750.7
SMILES Code [H][C@@]12CC3=C(Br)NC4=CC=CC(C1=C[C@@H](C(N[C@@]5(C(C)C)C(N6[C@@H](CC(C)C)C(N7CCC[C@]7([C@]6(O)O5)[H])=O)=O)=O)CN2C)=C43.OS(=O)(C)=O
MDL No. MFCD09028065
别名 CB-154; Bromocriptine (mesylate); 2-Bromoergocryptine Mesylate
运输蓝冰
InChI Key NOJMTMIRQRDZMT-GSPXQYRGSA-N
Pubchem ID 31100
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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