Roxadustat(Synonyms: 罗沙司他; FG-4592)

发表于由

Roxadustat (Synonyms: 罗沙司他; FG-4592) 纯度: 99.68%

Roxadustat (FG-4592) 是一种口服 低氧诱导因子脯氨酰羟化酶 抑制剂 (HIF-PHI)，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。

Roxadustat(Synonyms: 罗沙司他; FG-4592)

Roxadustat Chemical Structure

CAS No. : 808118-40-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥605 In-stock
10 mg ￥550 In-stock
50 mg ￥1800 In-stock
100 mg ￥3000 In-stock
200 mg ￥4000 In-stock
500 mg ￥7000 In-stock
1 g ￥11000 In-stock
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

Roxadustat 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Glutamine Metabolism Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Breast Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library
  • Rare Diseases Drug Library

生物活性

Roxadustat is an oral hypoxia-inducible factor prolyl-hydroxylase inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin[1].

IC50 & Target

Hypoxia-inducible factor prolyl-hydroxylase[1]
体外研究
(In Vitro)

Roxadustat (5-50 μM; 6 hours) significantly inhibits TBHP-induced apoptosis in PC12 cells[2].
Roxadustat (50 μM; 6 hours) stabilizes HIF-1α protein expression in PC12 cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[2]

Cell Line: PC12 cells
Concentration: 5, 20, 50 μM
Incubation Time: 6 hours
Result: Significantly inhibited TBHP-induced apoptosis.

Western Blot Analysis[2]

Cell Line: PC12 cells
Concentration: 50 μM
Incubation Time: 6 hours
Result: stabilized HIF-1α protein expression.

体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 12-week female C57BL/6 mice[2]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; daily for 7 days
Result: Protected the survival of motor neurons and improved recovery from spinal cord injury.

Clinical Trial

分子量

352.34

Formula

C19H16N2O5
CAS 号

808118-40-3
中文名称

罗沙司他
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (283.82 mM)

H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8382 mL 14.1908 mL 28.3817 mL
5 mM 0.5676 mL 2.8382 mL 5.6763 mL
10 mM 0.2838 mL 1.4191 mL 2.8382 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.10 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.10 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 3.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Provenzano R, et al. Roxadustat (FG-4592) Versus Epoetin Alfa for Anemia in Patients Receiving MaintenanceHemodialysis: A Phase 2, Randomized, 6- to 19-Week, Open-Label, Active-Comparator, Dose-Ranging, Safety and Exploratory Efficacy Study. Am J Kidney Dis. 2016 Jun;67(6):912-24.

    [2]. Wu K, et al. Stabilization of HIF-1α by FG-4592 promotes functional recovery and neural protection in experimental spinal cord injury. Brain Res. 2016 Feb 1;1632:19-26.