1. GPCR/G Protein
    Neuronal Signaling
    Membrane Transporter/Ion Channel
  2. Melatonin Receptor
    5-HT Receptor
    P2X Receptor
    TRP Channel
    Sodium Channel
  3. Piromelatine

Piromelatine (Synonyms: Neu-P11)

Cat. No.: HY-105285 Purity: 99.21%
Handling Instructions

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.

For research use only. We do not sell to patients.

Piromelatine Chemical Structure

Piromelatine Chemical Structure

CAS No. : 946846-83-9

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 308 In-stock
Estimated Time of Arrival: December 31
5 mg USD 280 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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Description

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[1][2][3].

IC50 & Target[1][2]

MT1

 

MT2

 

5-HT1A Receptor

 

5-HT1D Receptor

 

5-HT2B Receptor

 

In Vivo

Piromelatine (20 mg/kg, ip, daily) treatment prevents insulin resistance induced by sleep restriction[1].
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].

Animal Model: Twenty four male Sprague-Dawley rats (3 months old, weighing 250-300 g)[1].
Dosage: 20 mg/kg.
Administration: IP, daily at 8:00 p.m.
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%).
Animal Model: Five groups of 12-wk-old rats (10/group)[2].
Dosage: 5-50 mg/kg.
Administration: Intraperitoneal injection in 18:00 every day.
Result: Plasma glucose was decreased significantly by 27.3%, 34.5% and 61.5%, respectively.
Animal Model: Male C57BL/6 J mice, weighing 22-26 g (10 weeks old; PSL mice)[3].
Dosage: 25, 50, or 100 mg/kg.
Administration: IP 1 h before assessment of thermal hyperalgesia and mechanical allodynia.
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.
Molecular Weight

312.32

Formula

C₁₇H₁₆N₂O₄

CAS No.

946846-83-9

SMILES

O=C(C1=CC(C=CO1)=O)NCCC2=CNC3=CC=C(OC)C=C23

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (800.46 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2018 mL 16.0092 mL 32.0184 mL
5 mM 0.6404 mL 3.2018 mL 6.4037 mL
10 mM 0.3202 mL 1.6009 mL 3.2018 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

*All of the co-solvents are provided by MCE.
References
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Keywords:

PiromelatineNeu-P11Melatonin Receptor5-HT ReceptorP2X ReceptorTRP ChannelSodium ChannelSerotonin Receptor5-hydroxytryptamine ReceptorP2XRsTransient receptor potential channelsNa channelsNa+ channelsInsulinPlasmaglucoseHDL-CsleepAlzheimer'sInhibitorinhibitorinhibit

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