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Postion:Product Catalog >Biochemical Engineering>Inhibitors>GPCR & G Protein>MT Receptor agonists>Ramelteon
Ramelteon
  • Ramelteon

Ramelteon NEW

Price $59 $80 $138
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Ramelteon CAS No.: 196597-26-9
Purity: 99.92% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameRamelteon
DescriptionRamelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.
Kinase AssaycDNA encoding the human MT1 gene is introduced into CHO cells. Cells are harvested at confluence in Ca2+ and Mg2+ free Hanks' balanced salt solution containing 5 mM EDTA and collected by centrifugation. Cells are homogenized in ice-cold 50 mM Tris–HCl buffer, washed twice, pelleted, and stored at -30°C until the binding assays are conducted. Test compound and 40 pM 2-[ 125I]melatonin are mixed with the thawed homogenate in a total volume of 1 mL and incubated at 25°C for 150 min. The reaction is terminated by addition of 3 mL of icecold buffer followed by vacuum filtration on a Whatman GF/B. The filter is washed twice and radioactivity is counted by a g-counter[1].
In vitroRamelteon 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 vivoRamelteon 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.
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationH2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 49 mg/mL (188.9 mM)
DMSO : 60 mg/mL (231.36 mM)
KeywordsTAK375 | rebound insomnia | Melatonin Receptor | Ramelteon | insomnia | MT2 | withdrawal symptom | MT1 | inhibit | discontinuation | Inhibitor | next-morning residual effect | oral | TAK 375
Inhibitors RelatedMelatonin
Related Compound LibrariesBioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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