Roxadustat (FG-4592) 是一种口服有效的低氧诱导因子 (HIF) 脯氨酰羟化酶 (PHD) 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。
生物活性 | Roxadustat is an orally activehypoxia-inducible factor (HIF) prolyl-hydroxylase (PHD)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].
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. |
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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].
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. |
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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 |
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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 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 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-CDin saline) Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution *以上所有助溶剂都可在本网站选购。
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