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Piribedil dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Piribedil dihydrochloride图片
CAS NO:1451048-94-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
盐酸吡贝地尔;盐酸双哌嘧啶;盐酸泰舒达
产品介绍
Piribedil dihydrochloride 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 dihydrochloride 也是一种 α2-肾上腺素受体 (α2-adrenoceptors) 拮抗剂。Piribedil dihydrochloride 可抑制 MLL1 甲基转移酶的活性 (EC50: 0.18 μM)。Piribedil dihydrochloride 可用于研究帕金森病,循环系统疾病,癌症。
生物活性

Piribedil dihydrochloride is a potent and orally activedopamine D2anddopamine D3agonist. Piribedil dihydrochloride is also aα2-adrenoceptorsantagonist. Piribedil dihydrochloride can inhibitMLL1methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].

IC50& Target[1]

D2Receptor

 

D3Receptor

 

体外研究
(In Vitro)

Piribedil dihydrochloride (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation[4].
Piribedil dihydrochloride (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[4].
Piribedil dihydrochloride (0-160 μM, 4 days) induces cell-cycle arrest, apoptosis and differentiation in MLL-r cells (THP-1 and MV4;11)[4].

Cell Viability Assay[4]

Cell Line:MLL-r AML cells (THP-1 and MV4;11), non-MLL leukemia cell line (K562)
Concentration:0, 20, 40, 80 and 160 μM
Incubation Time:0-7 days
Result:Inhibited the growth rate of the THP-1 and MV4;11 cells in a time-dependent manner.

Western Blot Analysis[4]

Cell Line:THP-1 and MV4;11 cells
Concentration:0, 20, 40, 80 and 160 μM
Incubation Time:4 days
Result:Decreased the levels of H3K4me2 and H3K4me3 without affecting the methylation of other histones, such as H3K79, H3K36 and H3K27.
体内研究
(In Vivo)

Piribedil dihydrochloride (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in a rat model of Parkinson’s disease[2].
Piribedil dihydrochloride (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets[3].
Piribedil dihydrochloride (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[4].

Animal Model:Rat model of Parkinson’s disease[2]
Dosage:5, 15, 40 mg/kg
Administration:Intraperitoneal injection, administered 5 min before administration of L-DOPA.
Result:Reduced turning behaviour and AD (axial dystonia), OD (orolingual dyskinesia) and FD (forelimb dyskinesia) at 5 and 40 mg/kg.
Increased LD (locomotive dyskinesias) at the 40 mg/kg.
Animal Model:Adult common marmosets[3]
Dosage:4-5 mg/kg
Administration:Oral gavage, daily for 2 weeks
Result:Increased vigilance and alertness and reversed the downregulation of preprotachykinin mRNA induced by MPTP in rostral and caudal striatum.
Clinical Trial
分子量

371.26

Formula

C16H20Cl2N4O2

CAS 号

1451048-94-4

中文名称

盐酸吡贝地尔;盐酸双哌嘧啶;盐酸泰舒达

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.