生物活性
Ramelteon (TAK-375)是melatonin受体激动剂，对褪黑激素MT1（IC50 = 28.5±8.55 pM）和MT2（20.1±9.25 pM）受体均具有高亲和力，并且相对于MT3受体具有选择性。
靶点信息
| MT1 receptor | MT receptor (chicken) | MT2 receptor | | |
| 14 pM(Ki) | 23.1 pM(Ki) | 112 pM(Ki) | | |
化学数据
| 目录号 | A10777 |
| 作用机制 | Agonist (激动剂) |
| M. Wt | 259.3 |
| Formula | C16H21NO2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 196597-26-9 |
| Synonyms | Rozerem, TAK-375, TAK375 |
| SMILES | CCC(=O)NCC[C@@H]1CCC2=C1C3=C(C=C2)OCC3 |
溶解度
| In vitro (25°C) | DMSO | 47 mg/mL (181.22 mM) |
| Water | Insoluble |
| Ethanol | 47 mg/mL (181.22 mM) |
| In vivo | 0.5% methylcellulose | 28 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 38.57 mL | 192.83 mL | 385.65 mL |
| 0.5 mM | 7.71 mL | 38.57 mL | 77.13 mL |
| 1 mM | 3.86 mL | 19.28 mL | 38.57 mL |
| 5 mM | 0.77 mL | 3.86 mL | 7.71 mL |
*The above data is based on the productmolecular weight 259.3 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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