Piribedil
Based on 1 publication(s) in Google Scholar
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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- Pureza: 99.92%
- No. CAS: 3605-01-4
- Fòrmula: C16H18N4O2
- Peso molecular:298.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Piribedil
MoreVer todos los productos específicos de isoformas Dopamine Receptor
MoreVer todos los productos específicos de isoformas Adrenergic Receptor
MoreVer todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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α adrenergic receptor |
D2 Receptor |
D3 Receptor |
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.
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Cell Line:MLL-r AML cells (THP-1 and MV4;11), non-MLL leukemia cell line (K562)
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Concentration:0, 20, 40, 80 and 160 μM
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Incubation Time:0-7 days
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Result:Inhibited the growth rate of the THP-1 and MV4;11 cells in a time-dependent manner.
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Cell Line:THP-1 and MV4;11 cells
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Concentration:0, 20, 40, 80 and 160 μM
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Incubation Time:4 days
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Result:Decreased the levels of H3K4me2 and H3K4me3 without affecting the methylation of other histones, such as H3K79, H3K36 and H3K27.
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.
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Animal Model:Rat model of Parkinson’s disease[2]
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Dosage:5, 15, 40 mg/kg
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Administration:intraperitoneal injection, administered 5 min before administration of L-DOPA.
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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.
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Animal Model:Adult common marmosets[3]
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Dosage:4-5 mg/kg
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Administration:Oral gavage, daily for 2 weeks
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Result:Increased vigilance and alertness and reversed the downregulation of preprotachykinin mRNA induced by MPTP in rostral and caudal striatum.
Chemical Information
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No. CAS 3605-01-4
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Appearance Solid
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Peso molecular 298.34
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Fòrmula C16H18N4O2
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Color White to off-white
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SMILES
C1(N2CCN(CC3=CC=C(OCO4)C4=C3)CC2)=NC=CC=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Most Recent
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Front Chem
Terazosin Analogs Targeting Pgk1 as Neuroprotective Agents: Design, Synthesis, and Evaluation. [Abstract]2022 Jul 26:10:906974. PMID: 35958233
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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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)
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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. [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]
Complete Stock Solution Preparation Table
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.
| 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 |
Piribedil Related Classifications
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