Piribedil hydrochloride

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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.

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Piribedil hydrochloride Estructura química

No. CAS : 78213-63-5

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Other In-stock Forms of Piribedil hydrochloride:

Piribedil

Other Forms of Piribedil hydrochloride:

Piribedil-d₈ In-stock
Piribedil In-stock
Piribedil dihydrochloride Obtener un presupuesto
Piribedil maleate Obtener un presupuesto

1 Publications Citing Use of MCE Piribedil hydrochloride

•Front Chem. 2022 Jul 26:10:906974.

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•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Dopamine Receptor:

Ver todas las isoformas

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

Ver todos los productos específicos de isoformas Adrenergic Receptor:

Ver todas las isoformas

α adrenergic receptor β adrenergic receptor

Ver todos los productos específicos de isoformas Histone Methyltransferase:

Ver todas las isoformas

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Descripciòn

IC₅₀ & Target^[1]

D₂ Receptor

D₃ Receptor

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].

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

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.

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].

MedChemExpress (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.

Peso molecular

334.80

Fòrmula

C₁₆H₁₉ClN₄O₂

No. CAS

78213-63-5

SMILES

[H]Cl.C1(N2CCN(CC3=CC=C(OCO4)C4=C3)CC2)=NC=CC=N1

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Sweet RD, et al. Piribedil, a dopamine agonist, in Parkinson's disease. Clin Pharmacol Ther. 1974 Dec;16(6):1077-82. [Content Brief]

[2]. Gerlach M, et al. The effect of piribedil on L-DOPA-induced dyskinesias in a rat model of Parkinson's disease: differential role of α(2) adrenergic mechanisms. J Neural Transm (Vienna). 2013 Jan;120(1):31-6.

[3]. Smith LA, Tet al. Repeated administration of piribedil induces less dyskinesia than L-dopa in MPTP-treated common marmosets: a behavioural and biochemical investigation. Mov Disord. 2002 Sep;17(5):887-901. [Content Brief]

[4]. Xiong Zhang, et al. Piribedil disrupts the MLL1-WDR5 interaction and sensitizes MLL-rearranged acute myeloid leukemia (AML) to doxorubicin-induced apoptosis. Cancer Lett. 2018 Sep 1;431:150-160. [Content Brief]