Eliglustat

製品コードS7852 バッチS785201

印刷

化学情報

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

240 mg/mL (593.26 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）

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 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。	6.000mg/ml (14.83mM)	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）はグルコシルセラミド合成酵素（GCS）を阻害し、それによりリソソームへのグルコシルセラミド流入負荷を軽減します。
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 this compound is highly specific. It 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.
in vivo	Preclinical studies in normal mice, rats and dogs with i.v. and oral administration of this compound demonstrates significant dose-related decreases in spleen, kidney and liver glucosylceramide content, consistent with prior observations with the palmitoyl homologue.In rodents, this compound is rapidly metabolized with a half-life of 15–45 minutes.

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

参考

https://pubmed.ncbi.nlm.nih.gov/22563139/
https://pubmed.ncbi.nlm.nih.gov/20574539/

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
Glucose-dependent glycosphingolipid biosynthesis fuels CD8+ T cell function and tumor control [ bioRxiv, 2024, 2024.10.10.617261]	PubMed: 39464161
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。