Roxadustat (FG-4592)
目录号：S1007 别名： ASP1517
Molecular Weight(MW): 352.34
Roxadustat (FG-4592)在无细胞试验中是一种HIF-α脯氨酰羟化酶抑制剂，并能稳定HIF-2，同时诱导EPO产生。Phase 3。
客户使用该产品的6个实验数据：
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Immunoblots showing dose-dependent HIF-1α stabilization in U2OS, HeLa and Hep3b (and HIF-2α) cells after 6 hours treatment with FG-4592.
Chem Sci, 2017, doi: 10.1039/C7SC02103H. Roxadustat (FG-4592) purchased from Selleck.
(A) The viability of the EpSCs in each group was detected by CCK-8 assays. The EpSCs were under the indicated conditions for 24 h. The viability of each group is shown as the mean±SD. *, P<0.05 versus the normoxia control group; #, P<0.05 versus the hypoxia control group. (B) Western blotting results showing that FG-4592 simulated hypoxia-induced increases in HIF-1α and PCNA expression.
Cell Physiol Biochem, 2018, 46(6):2460-2470. Roxadustat (FG-4592) purchased from Selleck.
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Blood urea nitrogen (A), serum creatinine (B) and serum cystatin C (C) levels. Data were presented as means ± SD (n = 8 in each group). (D) Representative images of periodic acid-Schiff staining (upper: ×100, lower: ×400) of kidneys. (E) Tubular injury score in mice. Data were presented asmeans ± SD of 10 random fields from each kidney (n = 8 in each group).
Clin Sci, 2018, 132(7):825-838. Roxadustat (FG-4592) purchased from Selleck.
(B and C) Luciferase reporter activity following treatment with CP-312 or known HIF inducers, FG-4592 and BAY 85-3934, in (B) HIF-1 MIA PaCa-2 and (C) HIF-2-specific PANC-1 luciferase reporter cell lines.
J Pharmacol Exp Ther, 2018, 364(1):87-96. Roxadustat (FG-4592) purchased from Selleck.
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Protein content of Hypoxia-inducible factor 1, alpha subunit (HIF-1α) of PC12 cells treated with tert-Butyl hydroperoxide (TBHP) and TBHP plus FG-4592.
Brain Res, 2016, 1632:19-26. Roxadustat (FG-4592) purchased from Selleck.
Roxadustat (FG-4592) increases the differentiation of ADMSCs in hypoxic conditions. Representative micrographs showing immunofluorescence of COL I(green) and HIF-1a(green), and DAPI-labelled nuclei(blue) in each group. All cells were detected at day 21 post-induction.
Cell Prolif, 2016, 49(2):173-84.. Roxadustat (FG-4592) purchased from Selleck.
产品安全说明书
HIF抑制剂选择性比较
生物活性
| 产品描述 | Roxadustat (FG-4592)在无细胞试验中是一种HIF-α脯氨酰羟化酶抑制剂，并能稳定HIF-2，同时诱导EPO产生。Phase 3。 | |||||||||||||||||||||||
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| 靶点 |
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| 体外研究 |
FG-4592是一种口服缺氧诱导因子（HIF）脯氨酰羟化酶抑制剂,在临床上用于治疗贫血。FG-4592稳定HIF的活动，HIF是细胞内转录因子，导致与红细胞相关基因，包括EPO，和参与铁代谢相关酶的激活。[1] |
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| Cell Data |
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推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
溶解度 (25°C)
| 体外 | DMSO | 70 mg/mL (198.67 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 5% DMSO+50% PEG 300+ddH2O |
11mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 352.34 |
|---|---|
| 化学式 | C19H16N2O5 |
| CAS号 | 808118-40-3 |
| 稳定性 | powder |
| in solvent | |
| 别名 | ASP1517 |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03303066 | Recruiting | Primary MDS Classified as Very Low Low or Intermediate Risk With <5% Blasts | FibroGen|AstraZeneca | June 6 2018 | Phase 2|Phase 3 |
| NCT03303066 | Recruiting | Primary MDS Classified as Very Low Low or Intermediate Risk With <5% Blasts | FibroGen|AstraZeneca | June 6 2018 | Phase 2|Phase 3 |
| NCT03263091 | Recruiting | Primary MDS (Very Low Low or Intermediate IPSS-R With <5% Blasts) | FibroGen|AstraZeneca | September 7 2017 | Phase 3 |
| NCT03263091 | Recruiting | Primary MDS (Very Low Low or Intermediate IPSS-R With <5% Blasts) | FibroGen|AstraZeneca | September 7 2017 | Phase 3 |
| NCT02952040 | Completed | Healthy Subjects | Astellas Pharma Inc|FibroGen | November 2016 | Phase 1 |
| NCT02952040 | Completed | Healthy Subjects | Astellas Pharma Inc|FibroGen | November 2016 | Phase 1 |
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
常见问题及建议解决方法
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问题 1：
Can you tell me what the half-life of the product is, please?
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回答：
The half-life of S1007 Roxadustat is around 12 hours. Please the reference below: https://www.ncbi.nlm.nih.gov/pubmed/26846333
