Elafibranor

製品コードS3720 バッチS372004

印刷

化学情報

Synonyms

GFT505

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₂₄O₄S

分子量

384.49

CAS No.

923978-27-2

Solubility (25°C)*

体外

DMSO

77 mg/mL (200.26 mM)

Ethanol

13 mg/mL (33.81 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 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。	3.850mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 77 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 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。	0.480mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.6 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	Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.
in vitro	GFT505 is a novel PPAR modulator that shows a preferential activity on PPAR-α and concomitant activity on PPAR-δ^[2].
in vivo	Elafibranor (GFT505) is a dual PPARα/δ agonist that has demonstrated efficacy in disease models of nonalcoholic fatty liver disease (NAFLD)/NASH and liver fibrosis. In the rat, this compound concentrated in the liver with limited extrahepatic exposure and underwent extensive enterohepatic cycling. It confers liver protection by acting on several pathways involved in NASH pathogenesis, reducing steatosis, inflammation, and fibrosis. This chemical improved liver dysfunction markers, decreased hepatic lipid accumulation, and inhibited proinflammatory (interleukin-1 beta, tumor necrosis factor alpha, and F4/80) and profibrotic (transforming growth factor beta, tissue inhibitor of metalloproteinase 2, collagen type I, alpha 1, and collagen type I, alpha 2) gene expression^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	hSKP-HPCs
	濃度	30 µM
	反応時間	24 h
	実験の流れ	Cells were treated with indicated concentration of this compound for 24 h.
動物実験	動物モデル	hApoE2 KI and hApoE2 KI/PPAR-α KO mice
	投薬量	30 mg/kg
	投与方法	oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/26874076/
https://pubmed.ncbi.nlm.nih.gov/23703580/
https://pubmed.ncbi.nlm.nih.gov/31028903/

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：

A new NRF2 activator for the treatment of human metabolic dysfunction-associated fatty liver disease [ JHEP Rep, 2023, 5(10):100845]	PubMed: 37663119
A new NRF2 activator for the treatment of human metabolic dysfunction-associated fatty liver disease [ JHEP Rep, 2023, 5(10):100845]	PubMed: 37663119

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。