Piromelatine
Based on 2 publication(s) in Google Scholar
Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
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- Purity: 99.70%
- CAS No.: 946846-83-9
- 화학식: C17H16N2O4
- 분자량:312.32
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Piromelatine
MoreAll 5-HT Receptor Isoforms
MoreAll P2X Receptor Isoforms
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Biological Activity
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MT1 |
MT2 |
P2X3 Receptor |
5-HT1A Receptor |
5-HT1D Receptor |
5-HT2B Receptor |
5-HT1A Receptor |
5-HT1D Receptor |
5-HT2B Receptor |
Piromelatine (5-50 mg/kg, ip, daily) decreases plasma glucose significantly[2].
Piromelatine (100 mg/kg) decreases thermal hyperalgesia and mechanical allodynia in PSL (partial sciatic nerve ligation) mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Twenty four male Sprague-Dawley rats (3 months old, weighing 250-300 g)[1].
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Dosage:20 mg/kg.
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Administration:IP, daily at 8:00 p.m.
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Result:Resulted in significantly decreased plasma glucose levels (6.670.35 mmol/L, 6.770.34 mmol/L vs. 8.27 0.38 mmol/L), and the plasma glucose levels of the two groups were even neared to that of the normal control group (6.07±0.35 mmol/L).
Resulted in a decrease in triglycerides and total cholesterol levels (51.8% and 43.0%, respectively) and an elevation in HDL-C level (increase of 32.4%).
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Animal Model:Five groups of 12-wk-old rats (10/group)[2].
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Dosage:5-50 mg/kg.
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Administration:Intraperitoneal injection in 18:00 every day.
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Result:Plasma glucose was decreased significantly by 27.3%, 34.5% and 61.5%, respectively.
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Animal Model:Male C57BL/6 J mice, weighing 22-26 g (10 weeks old; PSL mice)[3].
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Dosage:25, 50, or 100 mg/kg.
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Administration:IP 1 h before assessment of thermal hyperalgesia and mechanical allodynia.
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Result:Remarkably prolonged thermal latency (surgery×treatment interaction, F1,24=15.7, p<0.001; surgery×treatment×hours interaction, F5,120=3.0, p<0.05) and increased mechanical threshold (surgery×treatment interaction, F1,24=18.4, p<0.001; surgery× treatment×hours interaction, F5,120=2.6, p<0.05) for 4 h after administration of piromelatine to PSL mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 946846-83-9
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Appearance Solid
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분자량 312.32
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화학식 C17H16N2O4
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Color Light yellow to yellow
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SMILES
O=C(C1=CC(C=CO1)=O)NCCC2=CNC3=CC=C(OC)C=C23
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Synonyms
Neu-P11
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 Nov 6;16(1):9812. PMID: 41198646 -
Int J Endocrinol
Neu-P11 Improves Type 2 Diabetes Mellitus Immune Function by Inhibiting the Hippo Signaling Pathway. [Abstract]2025 Oct 13:2025:3385546. PMID: 41122104
용액&용해도
DMSO : 250 mg/mL (800.46 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.08 mg/mL (6.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
순도&문서
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Meihua She, et al. Piromelatine, a Novel Melatonin Receptor Agonist, Stabilizes Metabolic Profiles and Ameliorates Insulin Resistance in Chronic Sleep Restricted Rats. Eur J Pharmacol. 2014 Mar 15;727:60-5. [Content Brief]
[2]. L Huang, et al. Blood Pressure Reducing Effects of Piromelatine and Melatonin in Spontaneously Hypertensive Rats. Eur Rev Med Pharmacol Sci. 2013 Sep;17(18):2449-56. [Content Brief]
[3]. Yuan-Yuan Liu, et al. Piromelatine Exerts Antinociceptive Effect via Melatonin, Opioid, and 5HT1A Receptors and Hypnotic Effect via Melatonin Receptors in a Mouse Model of Neuropathic Pain. Psychopharmacology (Berl). 2014 Oct;231(20):3973-85. [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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2018 mL | 16.0092 mL | 32.0184 mL | 80.0461 mL |
| 5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | 16.0092 mL | |
| 10 mM | 0.3202 mL | 1.6009 mL | 3.2018 mL | 8.0046 mL | |
| 15 mM | 0.2135 mL | 1.0673 mL | 2.1346 mL | 5.3364 mL | |
| 20 mM | 0.1601 mL | 0.8005 mL | 1.6009 mL | 4.0023 mL | |
| 25 mM | 0.1281 mL | 0.6404 mL | 1.2807 mL | 3.2018 mL | |
| 30 mM | 0.1067 mL | 0.5336 mL | 1.0673 mL | 2.6682 mL | |
| 40 mM | 0.0800 mL | 0.4002 mL | 0.8005 mL | 2.0012 mL | |
| 50 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6009 mL | |
| 60 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3341 mL | |
| 80 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0006 mL | |
| 100 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL |
Piromelatine Related Classifications
HY-105285 Related Classifications
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