TAK 375

Product Description

TAK 375 is a very high affinity and selective melatonin agonist (K_i 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.

Solubility

Preparing Stock Solutions for TAK 375

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Hirai Ramelteon (TAK-375) accelerates reentrainment of circadian rhythm after a phase advance of the light-dark cycle in rats J.Biol.Rhythms. 2005 PMID: 15654068
• Kato Neurochemical properties of rame. (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology. 2005 PMID: 15695169
• Stroethoff Melatonin receptor agonist rame. reduces ischemia-reperfusion injury through activation of mitochondrial potassium channels. J.Cardiovasc.Pharmacol. 2018 PMID: 29787401