标签归档：roxadustat

Roxadustat-d5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Roxadustat-d5 

Roxadustat-d5 是 Roxadustat 氘代物。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-d5

Roxadustat-d5 Chemical Structure

CAS No. : 2043026-13-5

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生物活性

Roxadustat-d5 is deuterium labeled Roxadustat. 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].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

357.37

Formula

C19H11D5N2O5
CAS 号

2043026-13-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. 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.

    [3]. 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.

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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
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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.