Roxadustat (FG-4592)

製品コードS1007 バッチS100706

印刷

化学情報

Synonyms

ASP1517

Storage
(From the date of receipt)

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

化学式

C₁₉H₁₆N₂O₅

分子量

352.34

CAS No.

808118-40-3

Solubility (25°C)*

体外

DMSO

70 mg/mL (198.67 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 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。	2.000mg/ml (5.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 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	Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Roxadustat potentiates RSL3 induced ferroptosis. Phase 3.
in vitro	Roxadustat (FG-4592) is an oral inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase currently in clinical development for the treatment of anemia. It stabilizes the activities of HIF, a cytosolic transcription factor, leading to activation of the genes associated with erythropoiesis, including erythropoietin and enzymes involved in iron metabolism. ^[1]
in vivo	Roxadustat (FG-4592) (50 mg/kg; i.p.; daily for 7 days) protects the survival of motor neurons and improves recovery from spinal cord injury.^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PC12 cells
	濃度	50 μM
	反応時間	6 h
	実験の流れ	After pre-treatment with FG-4592 alone or in combination with YC-1 for 6 h, cell cultures were immediately replenished with fresh medium containing 150 mM TBHP.
動物実験	動物モデル	Female C57BL/6 mice
	投薬量	50 mg/kg
	投与方法	i.p.

参考

http://worldwide.espacenet.com/publicationDetails/description?CC=US&NR=2007292433A1&KC=A1&FT=D&ND=3&
https://pubmed.ncbi.nlm.nih.gov/26707978/

カスタマーフィードバック

: Data from [Data independently produced by , , Chem Sci, 2017, doi: 10.1039/C7SC02103H]

: Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 46(6):2460-2470]

: Data from [Data independently produced by , , Clin Sci, 2018, 132(7):825-838]

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：

Immunothrombolytic monocyte-neutrophil axes dominate the single-cell landscape of human thrombosis and correlate with thrombus resolution [ Immunity, 2025, S1074-7613(25)00139-6]	PubMed: 40280129
Hypoxia promotes airway differentiation in the human lung epithelium [ Cell Stem Cell, 2025, S1934-5909(25)00338-8]	PubMed: 41075787
HIF-independent oxygen sensing via KDM6A regulates ferroptosis [ Mol Cell, 2025, 85(15):2973-2987.e6]	PubMed: 40712585
In Vitro and Ex Vivo Evidences that Pharmacological Induction of the Hypoxia Response Pathway Efficiently Restricts Measles and Nipah Virus Infections [ Emerg Microbes Infect, 2025, 2563067]	PubMed: 40958637
Roxadustat regulates the cell cycle and inhibits proliferation of mesangial cells via the hypoxia-inducible factor-1α/P53/P21 pathway [ Front Cell Dev Biol, 2025, 13:1503477]	PubMed: 40040789
Cystic fibrosis airway epithelial cells have an exaggerated response to hypoxia that is partially reversible through transmembrane receptor modulation [ J Cyst Fibros, 2025, S1569-1993(25)01561-9]	PubMed: 40816946
CRISPR-Cas9 genetic screens reveal regulation of TMPRSS2 by the Elongin BC-VHL complex [ Sci Rep, 2025, 15(1):11907]	PubMed: 40195420
Hypoxia-inducible factor 2α overexpression in podocytes ameliorates lipid metabolism disorders in diabetic kidney disease by inhibiting S1P [ Ren Fail, 2025, 47(1):2568972]	PubMed: 41077842
Roxadustat alleviates cisplatin-induced acute kidney injury by regulating fatty acid oxidation and mitochondrial function [ Ren Fail, 2025, 47(1):2561218]	PubMed: 40968500
Inherent single-cell heterogeneity of the transcriptional response to hypoxia in cancer cells [ NAR Cancer, 2025, 7(3):zcaf021]	PubMed: 40918648

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。