Ramelteon

SKU: orb1308555

Description

Ramelteon (TAK-375) is a selective agonist for melatonin MT1 and MT2 receptors. It is widely used in sleep research to investigate circadian rhythm regulation and sleep-wake cycles in both in vitro binding assays and in vivo animal models of insomnia.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 196597-26-9
• MW: 259.34
• Purity: 97.21% (May vary between batches)
• Formula: C₁₆H₂₁NO₂
• SMILES: CCC(=O)NCC[C@@H]1CCc2ccc3OCCc3c12
• Target: Melatonin Receptor,MT Receptor
• Solubility: Ethanol:49 mg/mL (188.94 mM);DMSO:60 mg/mL (231.36 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.71 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  MT receptor (chicken):23.1 pM(Ki)|MT2 receptor:112 pM(Ki)|MT1 receptor:14 pM(Ki)
• In Vivo:
  Ramelteon inhibited melanocyte pigment granule aggregation in the African clawed toad (Xenopus laevis) with a pEC50 of 11.48.1 nM Ramelteon increased ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells, but also in cerebellar granule cells containing only one melatonin receptor.Ramelteon inhibits forskolin-stimulated cAMP production with an IC50 of 21.2 pM in CHO cells. 4P-PDOT blocked the stimulatory effect of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, whereas luzindole attenuated the effect of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon showed high affinity for recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively.
• In Vitro:
  Ramelteon inhibited melanocyte pigment granule aggregation in the African clawed toad (Xenopus laevis) with a pEC50 of 11.48.1 nM Ramelteon increased ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells, but also in cerebellar granule cells containing only one melatonin receptor.Ramelteon inhibits forskolin-stimulated cAMP production with an IC50 of 21.2 pM in CHO cells. 4P-PDOT blocked the stimulatory effect of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, whereas luzindole attenuated the effect of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon showed high affinity for recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MTReceptor, MT2, MT2 receptor, MT1, MT receptor (chicken), MT Receptor, MT1 receptor, inhibit, next-morning residual effect, oral, insomnia, Inhibitor, MelatoninReceptor, Melatonin Receptor, discontinuation, TAK 375, TAK375, TAK-375, Ramelteon, withdrawal symptom, rebound insomnia

Compound Identifiers

PubChem CID

208902