Art. -Nr.: HY-12707

Piribedil

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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 (EC₅₀: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.

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Reinheit: 99.92%
CAS. Nr.: 3605-01-4
Formel: C₁₆H₁₈N₄O₂
Molecular Weight:298.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Piribedil Chemical Structure

CAS. Nr.: 3605-01-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

α adrenergic receptor

D₂ Receptor

D₃ Receptor

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

Piribedil (0-160 μM, 7 days) specifically inhibits MLL1 methyltransferase activity and selectively suppresses MLL-r cell proliferation^[4].
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^[4].
Piribedil (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 (intraperitoneal injection, 5, 15, 40 mg/kg ) alleviates the L-DOPA-induced dyskinesias in a rat model of Parkinson’s disease^[2].
Piribedil (oral gavage, 4-5 mg/kg, daily for 2 weeks) increases locomotor activity and reversal of motor deficits in adult common marmosets^[3].
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^[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.

Chemical Information

CAS. Nr. 3605-01-4
Appearance Solid
Molecular Weight 298.34
Formel C₁₆H₁₈N₄O₂
Color White to off-white
SMILES

C1(N2CCN(CC3=CC=C(OCO4)C4=C3)CC2)=NC=CC=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

Front Chem

Terazosin Analogs Targeting Pgk1 as Neuroprotective Agents: Design, Synthesis, and Evaluation. [Abstract]

2022 Jul 26:10:906974. PMID: 35958233

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 33.33 mg/mL (111.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3519 mL

16.7594 mL

33.5188 mL

5 mM

0.6704 mL

3.3519 mL

6.7038 mL

10 mM

0.3352 mL

1.6759 mL

3.3519 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3519 mL	16.7594 mL	33.5188 mL	83.7970 mL
	5 mM	0.6704 mL	3.3519 mL	6.7038 mL	16.7594 mL
	10 mM	0.3352 mL	1.6759 mL	3.3519 mL	8.3797 mL
	15 mM	0.2235 mL	1.1173 mL	2.2346 mL	5.5865 mL
	20 mM	0.1676 mL	0.8380 mL	1.6759 mL	4.1899 mL
	25 mM	0.1341 mL	0.6704 mL	1.3408 mL	3.3519 mL
	30 mM	0.1117 mL	0.5586 mL	1.1173 mL	2.7932 mL
	40 mM	0.0838 mL	0.4190 mL	0.8380 mL	2.0949 mL
	50 mM	0.0670 mL	0.3352 mL	0.6704 mL	1.6759 mL
	60 mM	0.0559 mL	0.2793 mL	0.5586 mL	1.3966 mL
	80 mM	0.0419 mL	0.2095 mL	0.4190 mL	1.0475 mL
	100 mM	0.0335 mL	0.1676 mL	0.3352 mL	0.8380 mL

Keywords

Piribedil

1 Cited Publications

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Piribedil

Epigenetics Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Endocrinology Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Anti-Blood Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

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Human Metabolite Library

Heterocyclic Compound Library

Pain-Related Compound Library

Off-patent Drug Library

Antihypertensive Compound Library

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Dopamine Receptor Compound Library

Anti-Hematopathy Compound Library

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FDA-Approved Drug Library Mini

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Piribedil

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Piribedil Related Classifications

HY-12707 Related Classifications