Delamanid

製品コードS5007 バッチS500704

印刷

化学情報

Chemical Structure Synonyms OPC-67683 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H25F3N4O6
分子量 534.48 CAS No. 681492-22-8
Solubility (25°C)* 体外 DMSO 21 mg/mL (39.29 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）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.35mg/ml 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. 
Clear solution
5% DMSO 95% Corn oil
0.26mg/ml Taking the 1 mL working solution as an example, add 50 μL of 5.2 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 Delamanid (OPC-67683) is a new anti-tuberculosis drug with an excellent intracellular bactericidal activity and a high accumulation rate.
in vitro

Delamanid potently inhibits the synthesis of mycolic acid, a long-chain fatty acid of the M. tuberculosis (mycobacterium tuberculosis) cell wall. Delamanid at concentrations of less than 5 μM shows no inhibitory effects on the efflux ABC transporters P-gp, BCRP, and BSEP or on the hepatic or renal SLC transporters OATPs, OCTs, and OATs. Delamanid is not metabolized by NADPH-dependent reactions, including those catalyzed by CYP enzymes, in human or animal liver microsomes. Also, delamanid has no inhibitory effects on the metabolism of exogenous CYP substrate compounds by eight CYP isoforms (CYP1A2, CYP2A6, CYP2B6, CYP2C8/9, CYP2C19, CYP2D6, CYP2E1, and CYP3A), even at a concentration of 100 μmol/liter, well above the therapeutic concentration[1].
in vivo

The water solubility of delamanid is poor and its absorption is increased more than two-fold by coadministration with food. The absolute bioavailability is unknown but estimated to be between 25% and 47%. In vivo, delamanid is more than 99% protein bound, with a high volume of distribution (Vz/F of 2100 L) and a half-life of 30-38 hours. Delamanid is excreted primarily in the stool, with less than 5% excretion in the urine. It is thought to be primarily metabolized by albumin, with secondary contributions from P450 enzymes, primarily CYP3A4. Animal studies indicate that delamanid is excreted in breast milk[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Leishmania donovani
濃度 15.5 nM
反応時間 24 h
実験の流れ

The parasites were treated with various concentrations of the drug for 24 h.
動物実験 動物モデル Female BALB/c mice
投薬量 1, 3, 10, 30 or 50 mg/kg
投与方法 p.o.

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：

Wollamide Cyclic Hexapeptides Synergize with Established and New Tuberculosis Antibiotics in Targeting Mycobacterium tuberculosis [ Microbiol Spectr, 2023, e0046523.] PubMed: 37289062
The Activities and Secretion of Cytokines Caused by Delamanid on Macrophages Infected by Multidrug-Resistant Mycobacterium tuberculosis Strains [ Front Immunol, 2021, 12:796677] PubMed: 35003120

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。