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Roxadustat

Cat. No. 7486 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
Pricing Availability   Qty
说明： HIF-PH inhibitor; erythropoietic
别名： FG 4592
化学名： N-[(4-Hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]glycine
纯度： ≥98% (HPLC)
说明书
引用文献
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生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Roxadustat

Roxadustat is a hypoxia-inducible factor prolyl hydroxylase enzyme (HIF-PH) inhibitor (IC50 = 591.4 nM). Roxadustat reduces basal oxygen consumption and increases glycolysis in vitro. It increases hemoglobin levels and stimulates erythropoiesis in vivo. By reducing ACE2 expression, roxadustat reduces the levels of SARS-CoV-2 viral RNA and inhibits entry, replication and secretion of infectious particles in lung epithelial cells. Roxadustat also suppresses hydroxylation and secretion of high molecular weight forms of mannose-binding lectin. The compound suppresses ion currents in pituitary tumor cells (IC50 values for inhibition of peak and late components of delayed rectifier calcium currents are 5.71 and 1.32 μM, respectively). Orally bioavailable.

技术数据 for Roxadustat

分子量 352.35
公式 C19H16N2O5
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 808118-40-3
PubChem ID 11256664
InChI Key YOZBGTLTNGAVFU-UHFFFAOYSA-N
Smiles O=C(O)CNC(=O)C=1N=C(C=2C=C(OC=3C=CC=CC3)C=CC2C1O)C

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Roxadustat

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 35.23 100

制备储备液 for Roxadustat

以下数据基于产品分子量 352.35。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.84 mL 14.19 mL 28.38 mL
5 mM 0.57 mL 2.84 mL 5.68 mL
10 mM 0.28 mL 1.42 mL 2.84 mL
50 mM 0.06 mL 0.28 mL 0.57 mL

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产品说明书 for Roxadustat

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for Roxadustat

参考文献是支持产品生物活性的出版物。

Chang et al (2019) Evidence for the capability of roxadustat (FG-4592), an oral HIF prolyl-hydroxylase inhibitor, to perturb membrane ionic currents:an unidentified yet important action. Int.J.Mol.Sci. 20 6027 PMID: 31795416

Wu et al (2018) Click chemistry-based discovery of [3-Hydroxy-5-(1H-1,2,3-triazol-4-yl)picolinoyl]glycines as orally active hypoxia-inducing factor prolyl hydroxylase inhibitors with favorable safety profiles for the treatment of anemia. J.Med.Chem. 61 5332

Jain et al (2016) Hypoxia as a therapy for mitochondrial disease. Science 352 54 PMID: 26917594

Bhute et al (2020) Mannose binding lectin is hydroxylated by collagen prolyl-4-hydroxylase and inhibited by some PHD inhibitors. Kidney360 2

Provenzano et al (2016) Oral hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat (FG-4592) for the treatment of anemia in patients with CKD. Clin.J.Am.Soc.Nephrol. 11 982 PMID: 27094610

If you know of a relevant reference for Roxadustat, please let us know.

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关键词: Roxadustat, Roxadustat supplier, FG4592, hypoxia, hydroxylase, inhibitors, erythropoiesis, ion, channels, currents, HIF, hemoglobin, virus, viral, ACE2, FG, 4592, Hydroxylases, Voltage-Gated, Potassium, Channels, 7486, Tocris Bioscience

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