Eliglustat

製品コードS7852 バッチS785201

印刷

化学情報

Chemical Structure Synonyms GENZ-112638 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H36N2O4
分子量 404.54 CAS No. 491833-29-5
Solubility (25°C)* 体外 DMSO 80 mg/mL (197.75 mM)
Ethanol 80 mg/mL (197.75 mM)
Water 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 Corn oil
6.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 120 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 Eliglustat (GENZ-112638) inhibits glucosylceramide synthase(GCS),thus reducing the load of glucosylceramide influx into the lysosome.
in vitro Eliglustat tartrate is designed and developed to inhibit glucosylceramide synthase, the enzyme that catalyzes the formation of glucosylceramide from UDP-glucose and ceramide.The inhibition of glucosylceramide synthase by eliglustat tartrate is highly specific. Eliglustat tartrate displays limited or no activity against a variety of glycosidases. Additionally, no inhibition of sucrase or maltase is observed at drug concentrations up to 10 μM[1].
in vivo Preclinical studies in normal mice, rats and dogs with i.v. and oral administration demonstrates significant dose-related decreases in spleen, kidney and liver glucosylceramide content, consistent with prior observations with the palmitoyl homologue[1].In rodents, Genz-112638 is rapidly metabolized with a half-life of 15–45 minutes[2].

プロトコル(参考用のみ)

動物実験 動物モデル DIO mice
投薬量 75 or 150mg/kg
投与方法 daily oral gavage

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：

Eliglustat exerts anti-fibrotic effects by activating SREBP2 in TGF-β1-treated myofibroblasts derived from patients with idiopathic pulmonary fibrosis [ Eur J Pharmacol, 2024, 966:176366] PubMed: 38296153
Glucosylceramide Synthase Inhibitors Induce Ceramide Accumulation and Sensitize H3K27 Mutant Diffuse Midline Glioma to Irradiation [ Int J Mol Sci, 2023, 24(12)9905] PubMed: 37373053
Tyrosine-phosphorylation and activation of glucosylceramide synthase by v-Src: Its role in survival of HeLa cells against ceramide [ Biochim Biophys Acta Mol Cell Biol Lipids, 2021, 1866(1):158817] PubMed: 32980536
Amyloid Beta-Peptide 25-35 (Aβ25-35) Induces Cytotoxicity via Multiple Mechanisms: Roles of the Inhibition of Glucosylceramide Synthase by Aβ25-35 and Its Protection by D609 [ Biol Pharm Bull, 2021, 44(10):1419-1426] PubMed: 34602551
N-Glycan Modification in Covid-19 Pathophysiology: In vitro Structural Changes with Limited Functional Effects [ J Clin Immunol, 2020, 1-10] PubMed: 33245474

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。