| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
| Targets |
D2/D3 Receptor
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|---|---|
| ln Vitro |
Piribedil (0-160 μM, 7 days) inhibits MLL1 methyltransferase activity in a particular manner and inhibits MLL-r cell growth in a targeted manner [4]. Piribedil (0-160 μM, 4 days) specifically inhibits the MLL1-WDR5 interaction, hence reducing H3K4 methylation in MLL-r cells (THP-1 and MV4; 11). MLL-r cells (THP-1 and MV4; 11) undergo cell cycle arrest, apoptosis, and differentiation when exposed to piribedil (0-160 μM) for four days [4].
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| ln Vivo |
Piribedil (intraperitoneal injection, 5, 15, 40 mg/kg) reduces levodopa-induced dyskinesia in a rat model of Parkinson's disease [2]. Pirbedil (oral gavage, 4-5 mg/kg daily for 2 weeks) increases locomotor activity and reverses motor deficits in adult common marmosets [3]. Piribedil (150 mg/kg orally, daily for 21 days) inhibits MLL-r tumor growth and reduces MLL1 target gene expression in MV4;11 tumor xenografts [4].
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| Enzyme Assay |
Targeting WT MLL for the treatment of MLL-r leukemia, which is highly aggressive and resistant to chemotherapy, has been shown to be a promising strategy. However, drug treatments targeting WT MLL are lacking. We used an in vitro histone methyltransferase assay to screen a library consists of 592 FDA-approved drugs for MLL1 inhibitors by measuring alterations in HTRF signal and found that Piribedil represented a potent activity. Piribedil specifically inhibited the proliferation of MLL-r cells by inducing cell-cycle arrest, apoptosis and myeloid differentiation with little toxicity to the non-MLL cells. Mechanism study showed Piribedil blocked the MLL1-WDR5 interaction and thus selectively reduced MLL1-dependent H3K4 methylation. Importantly, MLL1 depletion induced gene expression that was similar to that induced by Piribedil and rendered the MLL-r cells resistant to Piribedil-induced toxicity, revealing Piribedil exerted anti-leukemia effects by targeting MLL1. Furthermore, both the Piribedil treatment and MLL1 depletion sensitized the MLL-r cells to doxorubicin-induced apoptosis. Our study support the hypothesis that Piribedil could serve as a new drug for the treatment of MLL-r AML and provide new insight for further optimization of targeting MLL1 HMT activity.[4]
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| Cell Assay |
Cell proliferation assay[4]
Cell Types: MLL-r AML cells (THP-1 and MV4;11), non-MLL leukemia cell line (K562) Tested Concentrations: 0, 20, 40, 80 and 160 μM Incubation Duration: 0- 7 Experimental Results: Inhibited the growth rate of THP-1 and MV4;11 cells in a time-dependent manner. Western Blot Analysis[4] Cell Types: THP-1 and MV4; 11 cells Tested Concentrations: 0, 20, 40, 80 and 160 μM Incubation Duration: 4 days Experimental Results: H3K4me2 and H3K4me3 levels were diminished, but did not affect other histones Methylation, such as H3K79, H3K36 and H3K27. |
| Animal Protocol |
Animal/Disease Models: Parkinson's disease rat model [2]
Doses: 5, 15, 40 mg/kg Route of Administration: intraperitoneal (ip) injection, 5 minutes before levodopa administration. Experimental Results: Rotational behavior as well as AD (axial dystonia), OD (oral dyskinesia) and FD (forelimb dyskinesia) were diminished at doses of 5 and 40 mg/kg. LD (dyskinesia) increased at 40 mg/kg. Animal/Disease Models: Adult common marmoset [3] Doses: 4-5 mg/kg Route of Administration: po (oral gavage), one time/day for 2 weeks Experimental Results: Improved alertness and vigilance, reversed MPTP in rostral and caudal stripes Down-regulation of protachykinin mRNA induced in the cyst. |
| References |
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| Additional Infomation |
2-[4-(1,3-benzodioxol-5-ylmethyl)-1-piperazinyl]pyrimidine is a N-arylpiperazine.
Piribedil has been investigated in Parkinson's Disease. A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist. |
| Exact Mass |
298.142
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|---|---|
| Elemental Analysis |
C, 64.41; H, 6.08; N, 18.78; O, 10.73
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| CAS # |
3605-01-4
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| Related CAS # |
Piribedil-d8;1398044-45-5;Piribedil dihydrochloride;1451048-94-4;Piribedil hydrochloride;78213-63-5
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| PubChem CID |
4850
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
469.4±55.0 °C at 760 mmHg
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| Melting Point |
98 °C
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| Flash Point |
237.7±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.632
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| LogP |
2.36
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
356
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OQDPVLVUJFGPGQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H18N4O2/c1-4-17-16(18-5-1)20-8-6-19(7-9-20)11-13-2-3-14-15(10-13)22-12-21-14/h1-5,10H,6-9,11-12H2
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| Chemical Name |
2-(4-Piperonyl-1-piperazinyl)pyrimidine
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| Synonyms |
Piribedil; EU 4200; EU-4200; ET-495 ET 495; ET495; ET495; EU4200
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~111.72 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00591994 | COMPLETED | Drug: piribedil | Tinnitus | Faculdade de Medicina de Valenca | 2006-11 | Not Applicable |
| NCT00725478 | COMPLETED | Drug: Piribedil | Parkinson's Disease | Desitin Arzneimittel GmbH | 2008-01 | |
| NCT00727727 | COMPLETED | Drug: Piribedil | Parkinson's Disease | Desitin Arzneimittel GmbH | 2008-03 | |
| NCT01519856 | COMPLETED | Drug: piribedil (Clarium) | Parkinson's Disease | Desitin Arzneimittel GmbH | 2009-06 | |
| NCT01007864 | COMPLETED | Drug: piribedil Drug: pramipexole or ropinirole |
Idiopathic Parkinson's Disease | Desitin Arzneimittel GmbH | 2010-01 | Phase 3 |
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