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Roxadustat (FG-4592) 是一种口服生物可利用的缺氧诱导因子脯氨酰羟化酶抑制剂,通过增加内源性促红细胞生成素、改善铁调节和降低铁调素来促进红细胞生成,具有潜在的抗贫血活性。
Roxadustat (FG-4592) 是一种口服生物可利用的缺氧诱导因子脯氨酰羟化酶抑制剂,通过增加内源性促红细胞生成素、改善铁调节和降低铁调素来促进红细胞生成,具有潜在的抗贫血活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 179 | 现货 | |
5 mg | ¥ 283 | 现货 | |
10 mg | ¥ 336 | 现货 | |
25 mg | ¥ 493 | 现货 | |
50 mg | ¥ 628 | 现货 | |
100 mg | ¥ 917 | 现货 | |
500 mg | ¥ 2,270 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 315 | 现货 |
产品描述 | Roxadustat (FG-4592) is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity. |
体内活性 | FG-4592 (25 mg/kg) enhances mitophagy and attenuates retinal histopathologic damage in the photoreceptor layer after RD in an RD animal model[1]. |
激酶实验 | Kinase assays: Potencies (IC50 values) are determined by assays of active kinase domains cloned and expressed in baculovirus using the FastBacbaculovirus expression system or obtained commercially. For tyrosine kinase assays, a biotinylated peptide substrate containing a single tyrosine is used with 1 mM ATP, anEu-cryptate–labeled anti-phosphotyrosine antibody (PT66), and Strepavidin-APC in a homogeneous time-resolved fluorescence assay. Serine/threonine kinases are assayed using 5 μM ATP, [33P]ATP, and a biotinylated peptide substrate with peptide capture and incorporation of 33P determined using a SA-Flashplate. Linifanib is assayed at multiple concentrations prepared by serial dilution of a DMSO stock solution of Linifanib. The concentration resulting in 50% inhibition of activity is calculated using nonlinear regression analysis of the concentration response data. |
细胞实验 | The left eye of each rat is retro-orbitally injected with 25 mg/kg FG-4592 every 2 days, and an equal volume of 20% DMSO diluted with 0.9% NaCl is administrated with retro-orbital injection and served as the control. The retinae (attached, 1 day, 3 days, 5 days, and 7 days after RD) are homogenized and lysed with buffer containing 50 mM hydroxymethyl(Tris)-aminomethane(HCl), 150 mM NaCl, 1% Triton X-100, 1% sodium deoxycholate, 0.1% SDS, and a protease inhibitor tablet. Samples are run on 8% to 12% 2-hydroxyethyl (Bis)-hydroxymethyl (Tris) gel electrophoresis and transferred onto polyvinylidene difluoride (PVDF) membranes (0.2-mm pores). After blocking with 3% nonfat dried milk, the membranes are incubated overnight with primary antibody HIF-1α, LC3, BNIP3, autophagy-related gene 5 (Atg5), and β-actin. The blotted membranes are then incubated for 60 minutes at room temperature with a horseradish peroxidase (HRP)-labeled secondary antibody. Immunoreactive bands are visualized by enhanced chemiluminescence (ECL) and detected with an Amersham Imager 600. A minimum of three rats are used for each condition. |
别名 | 罗沙司他, FG-4592, ASP1517 |
分子量 | 352.34 |
分子式 | C19H16N2O5 |
CAS No. | 808118-40-3 |
Smiles | Cc1nc(C(=O)NCC(O)=O)c(O)c2ccc(Oc3ccccc3)cc12 |
密度 | 1.389 g/cm3 |
存储 | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 60 mg/mL (170.29 mM) | |||||||||||||||||||||||||||||||||||
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