2. GPCR/G Protein Neuronal Signaling Epigenetics
  3. Dopamine Receptor Adrenergic Receptor Histone Methyltransferase
  4. Piribedil hydrochloride

Piribedil hydrochloride  (Synonyms: 吡贝地尔盐酸盐；双哌嘧啶盐酸盐；泰舒达盐酸盐)

目录号: HY-12707C
产品使用指南

摩尔计算器

Piribedil hydrochloride 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 hydrochloride 也是一种 α2-肾上腺素受体 (α2-adrenoceptors) 拮抗剂。Piribedil hydrochloride 可抑制 MLL1 甲基转移酶的活性 (EC50: 0.18 μM)。Piribedil hydrochloride 可用于研究帕金森病，循环系统疾病，癌症。

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Piribedil hydrochloride Chemical Structure

Piribedil hydrochloride Chemical Structure

CAS No. : 78213-63-5

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Piribedil hydrochloride 的其他形式现货产品:

Customer Review

Other Forms of Piribedil hydrochloride:

Piribedil hydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Dopamine Receptor 亚型特异性产品:

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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α adrenergic receptor β adrenergic receptor

查看 Histone Methyltransferase 亚型特异性产品:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].

IC50 & Target[1]

D2 Receptor

 

D3 Receptor

 

体外研究
(In Vitro)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Piribedil hydrochloride 相关抗体:

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

334.80

Formula

C16H19ClN4O2
CAS 号
中文名称

吡贝地尔盐酸盐；双哌嘧啶盐酸盐；泰舒达盐酸盐
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.
纯度 & 产品资料
参考文献

Piribedil hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Piribedil78213-63-5吡贝地尔盐酸盐双哌嘧啶盐酸盐泰舒达盐酸盐Dopamine ReceptorAdrenergic ReceptorHistone MethyltransferaseBeta ReceptorParkinson'sdyskinesiaslocomotor activityanti-leukemicMLL1THP-1MV4;11leukemiacancerInhibitorinhibitorinhibit

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