| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Ramelteon (formerly TAK-375; TAK375; trade name: Rozerem), an approved medication used to treat sleeplessness / insomnia, is a melatonin receptor (MT) agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively. First of its kind, ramelteon selectively binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN), a novel class of sleep pharmaceuticals. The GABAA receptors, which are linked to amnesic, myorelaxant, and anxiolytic effects, do not exhibit any significant binding to ramelteon.
| Targets |
MT1 receptor ( Ki = 14 pM ); MT receptor (chicken) ( Ki = 23.1 pM ); MT2 receptor ( Ki = 112 pM )
|
||
|---|---|---|---|
| ln Vitro |
|
||
| ln Vivo |
|
||
| Enzyme Assay |
The human MT1 gene is inserted into CHO cells via cDNA. At confluence, cells are removed and collected by centrifugation in Hanks' balanced salt solution, which is free of calcium and magnesium and contains 5 mM EDTA. Before the binding tests are carried out, the cells are homogenized in an ice-cold 50 mM Tris-HCl buffer, twice cleaned, pelleted, and kept at -30°C. The thawed homogenate is combined with the test compound and 40 pM 2-[125I]melatonin in a volume of 1 mL, and it is then incubated for 150 minutes at 25°C. After adding 3 mL of ice-cold buffer and vacuum-filtering the mixture through a Whatman GF/B, the reaction is stopped. A g-counter is used to count the radioactivity after the filter has been cleaned twice.
|
||
| Cell Assay |
Ramelteon exhibits a very high affinity with Ki values of 14.0, 112, and 23.1 pM for chick forebrain melatonin receptors (comprising of melatonin1 and melatonin2 receptors) and human melatonin1 and melatonin2 receptors (expressed in CHO cells). Ramelteon's hamster brain melatonin3 binding site affinity is incredibly weak (Ki: 2.65 μM) in comparison to melatonin's (24.1 nM) affinity for the same binding site. Furthermore, there is no discernible affinity for any of the many ligand binding sites (benzodiazepine receptors, dopamine receptors, opiate receptors, ion channels, and transporters) or impact on the activity of different enzymes that ramelteon is supposed to inhibit. In CHO cells expressing human melatonin1 and melatonin2 receptors, ramelteon inhibits the production of cAMP stimulated by forskolin.
|
||
| Animal Protocol |
|
||
| References |
|
| Molecular Formula |
C16H21NO2
|
|---|---|
| Molecular Weight |
259.34
|
| Exact Mass |
259.16
|
| Elemental Analysis |
C, 74.10; H, 8.16; N, 5.40; O, 12.34
|
| CAS # |
196597-26-9
|
| Related CAS # |
Ramelteon-d3; 1432057-38-9; Ramelteon-d5; 1134159-63-9
|
| Appearance |
Solid powder
|
| SMILES |
CCC(=O)NCC[C@@H]1CCC2=C1C3=C(C=C2)OCC3
|
| InChi Key |
YLXDSYKOBKBWJQ-LBPRGKRZSA-N
|
| InChi Code |
InChI=1S/C16H21NO2/c1-2-15(18)17-9-7-12-4-3-11-5-6-14-13(16(11)12)8-10-19-14/h5-6,12H,2-4,7-10H2,1H3,(H,17,18)/t12-/m0/s1
|
| Chemical Name |
N-[2-[(8S)-2,6,7,8-tetrahydro-1H-cyclopenta[e][1]benzofuran-8-yl]ethyl]propanamide
|
| Synonyms |
TAK-375; TAK375; trade name: Rozerem; TAK 375
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8559 mL | 19.2797 mL | 38.5594 mL | |
| 5 mM | 0.7712 mL | 3.8559 mL | 7.7119 mL | |
| 10 mM | 0.3856 mL | 1.9280 mL | 3.8559 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02691013 | Active Recruiting |
Drug: Ramelteon Drug: Placebo |
Delirium Sleep Deprivation |
University of California, San Diego |
February 2016 | Not Applicable |
| NCT05069428 | Recruiting | Drug: Ramelteon 8mg | Delirium | Centennial Medical Center | March 26, 2023 | Phase 4 |
| NCT03091738 | Completed | Drug: Ramelteon Pill | Cirrhosis | Virginia Commonwealth University | February 1, 2017 | Phase 4 |
| NCT02669082 | Completed | Drug: Ramelteon | Insomnia Major Depressive Disorder |
Takeda | May 9, 2017 | Phase 4 |
| NCT01048242 | Completed | Drug: rozerem Drug: Placebo |
Insomnia Obstructive Sleep Apnea |
University of Pennsylvania | July 2006 | Phase 3 |
|
|---|
Blockade of ramelteon-induced potentiation of CREB phosphorylation by luzindole and forskolin.
Duration-dependent changes in insulin secretion during ramelteon treatment and after drug washout.PLoS One. 2014; 9(7): e102073 |
 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
