Tasimelteon

製品コードS4281 バッチS428101

印刷

化学情報

Synonyms

BMS 214778, VEC 162

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₅H₁₉NO₂

分子量

245.32

CAS No.

609799-22-6

Solubility (25°C)*

体外

DMSO

49 mg/mL (199.73 mM)

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 Corn oil

2.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Tasimelteon (BMS 214778, VEC 162) is a selective dual melatonin receptor (MT1/MT2) agonist with 2.1-4.4 times greater affinity for the MT2 receptor believed to mediate circadian rhythm phase-shifting (Ki = 0.0692 nM and Ki = 0.17 nM in NIH-3T3 and CHOeK1 cells, respectively), than for the MT1 receptor (Ki = 0.304 nM and Ki = 0.35 nM, respectively).
in vitro	Tasimelteon is a circadian regulator that resets the master clock in the suprachiasmatic nuclei of the hypothalamus by binding to both melatonin MT1 and MT2 receptors making it a dual melatonin receptor agonist^[3]. The affinity of tasimelteon for the MT2 receptor is 4-fold higher than its affinity for the MT1 receptor^[2].
in vivo	In rats and monkeys, the half-life of tasimelteon was approximately 2 h which is longer than the half-life of melatonin^[1]. Tasimelteon has a mean absolute bioavailability of approximately 38.3%. The higher oral-to-IV exposure ratios and decrease in the metabolite-to-parent ratios after IV administration for tasimelteon's metabolites indicate that although tasimelteon is subject to first-pass metabolism, a substantial fraction of its metabolism occurs post- rather than presystemically. Both oral and IV tasimelteon were well tolerated^[2].

プロトコル(参考用のみ)

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Melatonin Treatment Triggers Metabolic and Intracellular pH Imbalance in Glioblastoma [ Cells, 2022, 11(21)3467]	PubMed: 36359862

Melatonin Treatment Triggers Metabolic and Intracellular pH Imbalance in Glioblastoma [ Cells, 2022, 11(21)3467]

PubMed: 36359862

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。