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Piromelatine

Catalog No. T34081 CAS 946846-83-9

Synonyms: NEU-P-11, NEU-P 11, NEU-P11

Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.

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Piromelatine, CAS 946846-83-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 67.00
5 mg	In stock	$ 163.00
10 mg	In stock	$ 247.00
25 mg	In stock	$ 428.00
50 mg	In stock	$ 690.00
100 mg	In stock	$ 987.00
500 mg	In stock	$ 1,980.00
1 mL * 10 mM (in DMSO)	In stock	$ 178.00

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Purity: 100%

Biological Description

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Description

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.[3]

Synonyms	NEU-P-11, NEU-P 11, NEU-P11
Molecular Weight	312.32
Formula	C17H16N2O4
CAS No.	946846-83-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (320.18 mM), Sonication is recommended.

References and Literature

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. 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. 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. 4. Schneider LS, et al. A Polymorphism Cluster at the 2q12 locus May Predict Response to Piromelatine in Patients with Mild Alzheimer's Disease. J Prev Alzheimers Dis. 2022;9(2):247-254.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Drug Repurposing Compound Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Piromelatine 946846-83-9 GPCR/G Protein Membrane transporter/Ion channel Neuroscience P2X Receptor MT Receptor 5-HT Receptor Sodium Channel TRP/TRPV Channel NEU-P-11 NEU-P 11 NEU-P11 inhibitor inhibit

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