Piribedil|3605-01-4|(吡贝地尔; 双哌嘧啶)-陌孚医药/Medlife

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Piribedil (Synonyms: 吡贝地尔; 双哌嘧啶)

目录号: PL09201 纯度: ≥99%

Piribedil 是一种有效且具有口服活性的多巴胺 D2 (dopamine D2) 和多巴胺 D3 (dopamine D3) 激动剂。Piribedil 也是一种 α2-肾上腺素受体 (α2-adrenoceptors) 拮抗剂。Piribedil 可抑制 MLL1 甲基转移酶的活性 (EC50: 0.18 μM)。Piribedil 可用于研究帕金森病，循环系统疾病，癌症。

CAS No. :3605-01-4

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PL09201-1g	1g	¥6282.50	请登录
PL09201-5g	5g	询价	询价
PL09201-10mM*1mLinDMSO	10mM*1mLinDMSO	¥618.00	请登录

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中文名称	Piribedil
中文别名	吡贝地尔;2-[4-(1,3-苯并间二氧杂环戊烯-5-基甲基)哌嗪-1-基]嘧啶;比贝地尔;2-[4-(1,3-苯并二唑-5-基甲基)-1-哌嗪基]嘧啶;双哌嘧啶
英文名称	Piribedil
英文别名	2-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)pyrimidine;2[4-(1,3-benzodioxol-5-ylmethyl)-1-piperazinyl-]pyrimidine;Piribendyl;Piribedil;2-[4-(1,3-Benzodioxol-5-ylmethyl)-1-piperazinyl]pyrimidine;ET 495;EU-4200;Piribedile [DCIT];Piribedilum [INN-Latin];Trivastal;Trivastan;2-[4-(1,3-Benzodioxol-5-ylmethyl)piperazin-1-yl]pyrimidine;EU 4200;Piribedil [INN:DCF];DO22K1PRDJ;1-(2-Pyrimidyl)-4-piperonylpiperazine;2-(4-Piperonyl-1-piperazinyl)pyrimidine;Pyrimidine, 2-(4-piperonyl-1-piperazinyl)-;Pyrimidine, 2-[4-(1,3-benzodioxol-5-ylmethyl)-1-piperazinyl]-;OQDPVLVUJFGPGQ-UHFFFAOYSA-N
Cas No.	3605-01-4
分子式	C₁₆H₁₈N₄O₂
分子量	298.34
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Piribedil 是一种有效且具有口服活性的多巴胺 D2 (dopamine D2) 和多巴胺 D3 (dopamine D3) 激动剂。Piribedil 也是一种 α2-肾上腺素受体 (α2-adrenoceptors) 拮抗剂。Piribedil 可抑制 MLL1 甲基转移酶的活性 (EC₅₀: 0.18 μM)。Piribedil 可用于研究帕金森病，循环系统疾病，癌症。

生物活性

Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC 50 : 0.18 μM). Piribedil has the potential for the research of parkinsons disease, circulatory disorders, cancers.

性状

Solid

IC50 & Target[1][2]

D2 Receptor D3 Receptor

体外研究(In Vitro)

Piribedil (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation.
Piribedil (0-160 μM, 4 days) selectively decreases the H3K4 methylation in MLL-r cells (THP-1 and MV4;11), by disturbing the MLL1-WDR5 interaction.
Piribedil (0-160 μM, 4 days) induces cell-cycle arrest, apoptosis and differentiation in MLL-r cells (THP-1 and MV4;11).
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Piribedil (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in a rat model of Parkinson’s disease.
Piribedil (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets.
Piribedil (oral gavage, 150 mg/kg, daily for 21 days) inhibits MLL-r tumor growth and decreases the expression of MLL1 target genes in MV4;11 tumor xenografts. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Sweet RD, et al. Piribedil, a dopamine agonist, in Parkinsons disease. Clin Pharmacol Ther. 1974 Dec;16(6):1077-82.
[2]. Gerlach M, et al. The effect of piribedil on L-DOPA-induced dyskinesias in a rat model of Parkinsons disease: differential role of α(2) adrenergic mechanisms. J Neural Transm (Vienna). 2013 Jan;120(1):31-6.

溶解度数据	In Vitro: DMSO : 33.33 mg/mL (111.72 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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