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Very high affinity and selective melatonin agonist (Ki values are 14 and 112 pM for human MT1 and MT2, respectively). Selective for human MT1 and MT2 over hamster MT3 and a range of other targets including benzodiazepine, opiate and dopamine receptors, ion channels and transporters. Accelerates return to normal circadian rhythm in rats after phase shift, without affecting learning and memory. Also reduces infarct size in rat heart in vitro post ischemia-reperfusion.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 259.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.86 mL||19.28 mL||38.56 mL|
|5 mM||0.77 mL||3.86 mL||7.71 mL|
|10 mM||0.39 mL||1.93 mL||3.86 mL|
|50 mM||0.08 mL||0.39 mL||0.77 mL|
References are publications that support the biological activity of the product.
Stroethoff et al (2018) Melatonin receptor agonist rame. reduces ischemia-reperfusion injury through activation of mitochondrial potassium channels. J.Cardiovasc.Pharmacol. 72 106 PMID: 29787401
Hirai et al (2005) Ramelteon (TAK-375) accelerates reentrainment of circadian rhythm after a phase advance of the light-dark cycle in rats J.Biol.Rhythms. 20 27 PMID: 15654068
Kato et al (2005) Neurochemical properties of rame. (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology. 48 301 PMID: 15695169
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Keywords: TAK 375, TAK 375 supplier, TAK375, melatonin, receptor, agonists, agonism, selective, very, high, affinity, MT1, MT2, circadian, rhythm, Ramelteon, Melatonin, (MT), Receptors, 6777, Tocris Bioscience
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