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Roxadustat

Rating icon 很棒
产品编号 T2515Cas号 808118-40-3
别名 罗沙司他, FG-4592, ASP1517

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

Roxadustat

Rating icon 很棒
纯度: 99.94%
产品编号 T2515 别名 罗沙司他, FG-4592, ASP1517Cas号 808118-40-3

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
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纯度:99.94%
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产品介绍

生物活性
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
化学信息
分子量352.34
分子式C19H16N2O5
CAS No.808118-40-3
SmilesCc1nc(C(=O)NCC(O)=O)c(O)c2ccc(Oc3ccccc3)cc12
密度1.389 g/cm3
储存&溶解度
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)
溶液配制表
1mg5mg10mg50mg
1 mM2.8382 mL14.1908 mL28.3817 mL141.9084 mL
5 mM0.5676 mL2.8382 mL5.6763 mL28.3817 mL
10 mM0.2838 mL1.4191 mL2.8382 mL14.1908 mL
20 mM0.1419 mL0.7095 mL1.4191 mL7.0954 mL
50 mM0.0568 mL0.2838 mL0.5676 mL2.8382 mL
100 mM0.0284 mL0.1419 mL0.2838 mL1.4191 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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