Piromelatine

SKU: orb1695652

Description

Piromelatine is a multi-target small molecule acting as an MT1/MT2 and 5-HT1A/1D agonist and a 5-HT2B antagonist. Its research applications include studies of sleep, neuropathic pain, and depression, supported by in vivo models demonstrating antinociceptive, neuroprotective, and memory-enhancing effects.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 946846-83-9
• MW: 312.32
• Purity: >99.99% (May vary between batches)
• Formula: C₁₇H₁₆N₂O₄
• SMILES: COc1ccc2[nH]cc(CCNC(=O)c3cc(=O)cco3)c2c1
• Target: TRP/TRPV Channel,P2X Receptor,Sodium Channel,5-HT Receptor,MT Receptor,Melatonin Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (12.81 mM);DMSO:100 mg/mL (320.18 mM)

Bioactivity

• In Vivo:
  Piromelatine (Neu-P11) has been shown to inhibit weight gain and improve insulin sensitivity in high-fat/high-sucrose-fed (HFSD) rats. The objective of this study was to investigate the effects of piromelatine on insulin sensitivity in sleep-restricted rats. Sleep restriction was established by rotating cages intermittently for 20h thereby sleeping time of rats was limited to 4 hours per day. During 8 days of sleep restriction, rats were injected intraperitoneally with piromelatine (20mg/kg), melatonin (5mg/kg), or a vehicle. The results showed that sleep restriction increased plasma glucose, fasting insulin, total cholesterol (TC), triglycerides (TG), and oxidative stress markers while HDL-cholesterol (HDL-C) level and glucose tolerance were decreased. However, under piromelatine or melatonin treatment, the levels of plasma glucose, TG, and TC decreased and HDL-C, glucose tolerance, and antioxidative potency increased when compared with the vehicle-treated group. Piromelatine could regulate metabolic profiles and insulin sensitivity, and attenuate insulin resistance induced by sleep restriction.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TRPChannel, TRP Channel, TRPVChannel, TRPV Channel, TRPV1, Sodium Channel, SodiumChannel, Piromelatine, P2X3, P2X Receptor, P2XReceptor, MTReceptor, MT Receptor, MT1 receptor, MT2 receptor, Nav1.7 channel, NEU-P 11, NEU-P11, NEU-P-11, 5HTReceptor, 5-HT2B, 5-HT1D, 5-HT1A, 5HT Receptor

Compound Identifiers

PubChem CID

24815904