Tasimelteon (BMS-214778)

A melatonin receptor agonist

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库存: 现货

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5mg

￥550.00

440.00

- +
10mg

￥875.00

700.00

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50mg

￥2612.00

2090.00

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100mg

￥3887.00

3110.00

- +

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Background

Tasimelteon is a melatonin (MT) receptor agonist.¹ It selectively binds MT₁ and MT₂ receptors (K_is = 0.304 and 0.069 nM, respectively, in NIH3T3 cells expressing the recombinant human receptors) over a panel of 160 additional receptors and enzymes at 10 ?M. Tasimelteon inhibits forskolin-induced cAMP accumulation with EC₅₀ values of 0.79 and 1 nM in NIH3T3 cells expressing the MT₁ or MT₂ receptor, respectively. Formulations containing tasimelteon have been used in the treatment of non-24-hour sleep-wake disorder.

1.Lavedan, C., Forsberg, M., and Gentile, A.J.Tasimelteon: A selective and unique receptor binding profileNeuropharmacology91142-147(2015)