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Ramelteon

Catalog No. T1463Cas No. 196597-26-9
Alias TAK-375

Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.

Ramelteon

Ramelteon

Purity: 99.92%
Catalog No. T1463Alias TAK-375Cas No. 196597-26-9
Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.
Pack SizePriceAvailabilityQuantity
2 mg$37In Stock
5 mg$59In Stock
10 mg$80In Stock
25 mg$138In Stock
50 mg$213In Stock
100 mg$343In Stock
500 mg$539In Stock
1 mL x 10 mM (in DMSO)$65In Stock
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Purity:99.92%
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Product Introduction

Bioactivity
Description
Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.
Targets&IC50
MT1 receptor:14 pM(Ki), MT receptor (chicken):23.1 pM(Ki), MT2 receptor:112 pM(Ki)
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.
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.
Kinase Assay
cDNA 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].
AliasTAK-375
Chemical Properties
Molecular Weight259.34
FormulaC16H21NO2
Cas No.196597-26-9
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 49 mg/mL (188.9 mM)
DMSO: 60 mg/mL (231.36 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM3.8559 mL19.2797 mL38.5594 mL192.7971 mL
5 mM0.7712 mL3.8559 mL7.7119 mL38.5594 mL
10 mM0.3856 mL1.9280 mL3.8559 mL19.2797 mL
20 mM0.1928 mL0.9640 mL1.9280 mL9.6399 mL
50 mM0.0771 mL0.3856 mL0.7712 mL3.8559 mL
100 mM0.0386 mL0.1928 mL0.3856 mL1.9280 mL

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