Roxadustat (FG-4592)

製品コードS1007 バッチS100703

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
* <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	FG-4592 is an oral inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase currently in clinical development for the treatment of anemia. FG-4592 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 (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	Cell cultures were pre-treated with FG-4592 alone or in the presence of YC-1 for 6 h and then the culture medium was replaced immediately by fresh medium with 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

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：

Factor inhibiting HIF negatively regulates antiviral innate immunity via hydroxylation of IKKϵ [ Cell Rep, 2024, 43(1):113606.]	PubMed: 38127621
Inhibition of OGFOD1 by FG4592 confers neuroprotection by activating unfolded protein response and autophagy after ischemic stroke [ J Transl Med, 2024, 22(1):248]	PubMed: 38454480
The N6-methyladenosine demethylase ALKBH5 regulates the hypoxic HBV transcriptome [ PLoS Pathog, 2024, 20(1):e1011917]	PubMed: 38227578
Hypoxia-inducible factor upregulation by roxadustat attenuates drug reward by altering brain iron homoeostasis [ Signal Transduct Target Ther, 2023, 10.1038/s41392-023-01578-2]	PubMed: 37718358
Hypoxia-inducible factor upregulation by roxadustat attenuates drug reward by altering brain iron homoeostasis [ Signal Transduct Target Ther, 2023, 8(1):355]	PubMed: 37718358
Hypoxia stabilizes SETDB1 to maintain genome stability [ Nucleic Acids Res, 2023, gkad796]	PubMed: 37850636
Osteocyte Egln1/Phd2 links oxygen sensing and biomineralization via FGF23 [ Bone Res, 2023, 11(1):7]	PubMed: 36650133
Selective induction of human renal interstitial progenitor-like cell lineages from iPSCs reveals development of mesangial and EPO-producing cells [ Cell Rep, 2023, S2211-1247(23)01614-5]	PubMed: 38237600
Der Einfluss von Hypoxie auf Neutrophile Granulozyten und Neutrophile Extrazelluläre Fallen-Bildung [ Frontiers in-Immunology, 2023, ]	PubMed: None
Hypoxia Primes Human ISCs for Interleukin-Dependent Rescue of Stem Cell Activity [ Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.07.012]	PubMed: 37562653

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。