lurasidone

製品コードS5714 バッチS571401

印刷

化学情報

Synonyms

SM-13496

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₈H₃₆N₄O₂S

分子量

492.68

CAS No.

367514-87-2

Solubility (25°C)*

体外

DMSO

7 mg/mL (14.2 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 95 %Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.05mg/ml (0.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 1 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.35mg/ml (0.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. 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	lurasidone (SM-13496)は、ドパミンD2およびセロトニン5-HT2A受容体に対して完全な拮抗作用を示す第2世代抗精神病薬であり、それぞれ結合親和性Ki = 1 nMおよびKi = 0.5 nMです。また、セロトニン5-HT7受容体(Ki = 0.5 nM)に対して高い親和性を持ち、5-HT1A受容体(Ki = 6.4 nM)に対して部分アゴニスト活性を示し、ヒスタミンH1およびムスカリンM1受容体に対する親和性はありません。
in vitro	Lurasidone is a new atypical antipsychotic in the benzoisothiazoles class of chemicals. Like most second-generation antipsychotics it is a full antagonist at dopamine D2 and serotonin 5-HT2A receptors, and is a partial agonist at 5-HT1A receptors. It has much greater affinity for 5-HT7 subtype receptors than other atypical antipsychotics. This compound also has high affinity for the 5-HT1A subtype, α2c-adrenergic receptors and low affinity for α1-adrenergic receptors. It has minimal affinity for 5-HT2C receptors and negligible affinity for histamine H1 and muscarinic receptors.
in vivo	Lurasidone is rapidly absorbed, reaching peak concentrations within 1.5–3 hours (tmax) after single and multiple oral doses. Once absorbed, it extensively distributes in tissues and rapidly enters the CNS. This compound has high binding to human plasma albumin and alpha-1-glycoprotein (≥99%). Long-term treatment of schizophrenia with this agent has been shown to reduce the risk of relapse. The elimination half-life of this chemical is about 20-40 h. Mean Cmax and area under the curve (AUC) for this drug were approximately threefold and twofold greater, respectively, in a comparison of administration with food v. fasting. Its absorption is independent of food fat content. It is metabolised primarily via CYP3A4. In animal studies, this compound penetrated the placental barrier and distributed into the fetus, and was excreted in milk during lactation.

プロトコル(参考用のみ)

参考

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4706192/
https://pubmed.ncbi.nlm.nih.gov/22570547/

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：

Amisulpride as a potential disease-modifying drug in the treatment of tauopathies [ Alzheimers Dement, 2023, 10.1002/alz.13090]	PubMed: 37218673
A review on computer-aided chemogenomics and drug repositioning for rational COVID-19 drug discovery [ Chem Biol Drug Des, 2022, 100(5):699-721]	PubMed: 36002440
Exploring the kinetic selectivity of antipsychotics for dopamine D2 and 5-HT2A [ bioRxiv, 2021, 10.1101/2021.11.14.468520]	PubMed: None

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。