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

Piromelatine  (Synonyms: Neu-P11)

Cat. No.: HY-105285 Purity: 99.54%
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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

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Based on 1 publication(s) in Google Scholar

Piromelatine Related Antibodies

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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

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

312.32

Formula

C17H16N2O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 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

    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.
  • Protocol 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

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Piromelatine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Piromelatine946846-83-9Neu-P11Melatonin Receptor5-HT ReceptorP2X ReceptorTRP ChannelSodium ChannelSerotonin Receptor5-hydroxytryptamine ReceptorP2XRsTransient receptor potential channelsNa channelsNa+ channelsInsulinPlasmaglucoseHDL-CsleepAlzheimer'sInhibitorinhibitorinhibit

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