Ramelteon

貨號 Cat. No.: S1259
規格 Size: 10mM/1mL~50mg
品牌 Brand: Selleckchem

Description

Ramelteon

Catalog No.S12591 Product Citations

Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 352	In stock	0 1 2 3 4 5 6 7 8 9 10
2mg	USD 138	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 592	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 2104	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Biological Activity

Description	Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.
Targets	MT1 receptor	MT2 receptor	MT receptor (chicken)
IC50	14 pM (Ki)	112 pM (Ki)	23.1 pM (Ki) [1]
In vitro	Ramelteon inhibits forskolin-stimulated cAMP production with IC50 of 21.2 pM in CHO cells. [1] Ramelteon has high affinity with recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively. Ramelteon inhibits Xenopus laevis melanophore pigment granule aggregation with pEC50 of 11.48. [2]Ramelteon (1 nM) increases ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells but also in cerebellar granule cells expressing only one of the two melatonin receptors. 4P-PDOT blocks the stimulatory action of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, while luzindole attenuates the action of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon (100 μM) induces any pigment dispersion while melatonin completely disperses aggregated melanophores at 10 μM. [3]
In vivo	Ramelteon (10 mg/kg, i/p) significantly reduces NREM sleep latency in rat and also produces a short-lasting increase in nonrapid eye movement (NREM) sleep duration, but the NREM power spectrum is unaltered. [2]Ramelteon (0.1 mg/kg and 1 mg/kg, p.o.) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle in rats without affecting learning or memory. [4] Ramelteon (0.03 mg/kg and 0.3 mg/kg, p.o.) significantly shortens latency to sleep onset and significantly increases total duration of sleep in freely moving monkeys without affecting the general behavior of the monkeys. [5]
Features	A tricyclic synthetic analog of melatonin.

Protocol(Only for Reference)

Kinase Assay: [1]

Binding assays

Cells expressing the tested receptor are selected and cultured in Eagle’s Minimum Essential Medium-α (MEM-α) supplemented with 10% dialyzed fetal bovine serum (dFBS) under a 5% CO2/95% air atmosphere. Cells are harvested at confluence in Ca2+-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 (pH 7.7 at 25 â„ƒ), washed twice, pelleted, and stored at −30 â„ƒ until the binding assays are conducted. Ramelteon and 40 pM 2-[125I]melatonin are mixed with the thawed homogenate in a total volume of 1 mL and incubated at 25 â„ƒ for 150 min. The reaction is terminated by addition of 3 mL of ice-cold buffer followed by vacuum filtration on a Whatman GF/B. The filter is washed twice and radioactivity is counted by a γ-counter. Nonspecific binding is defined as the binding in the presence of 10 μM melatonin.

Animal Study: [4]

Animal Models	estrogen-deficient ovariectomized (OVX) rats
Dosages	1 mg/kg
Administration	Orally
Solubility	0.5% methylcellulose, 30 mg/mL

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Phases
NCT01677182	Recruiting	Bipolar Disorder	Takeda	Phase 3
NCT01685151	Withdrawn	Bipolar Disorder	Takeda	Phase 3
NCT01467713	Recruiting	Bipolar Disorder	Takeda	Phase 3
NCT01467700	Recruiting	Acute Depressive Episode	Takeda	Phase 3
NCT01207050	Recruiting	Insomnia\|Brain Injury	Kessler Foundation	Phase 4

Chemical Information

Download Ramelteon SDF

Molecular Weight (MW)	259.34
Formula	C16H21NO2
CAS No.	196597-26-9

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	Rozerem, TAK-375

Solubility (25°C) *	In vitro	DMSO	52 mg/mL (200 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	52 mg/mL (200 mM)
	In vivo	0.5% methylcellulose,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.