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5mg |
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50mg |
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Purity: ≥98%
Roxadustat (FG4592, ASP1517) is a novel, potent and orally bioavailable inhibitor of HIF-PH (hypoxia-inducible factor prolyl hydroxylase) with the potential to treat anemia associated with chronic kidney disease (CKD). HIF-PH is an enzyme that can up-regulate the expression of endogenous human erythropoietin (Epo). Roxadustat induces EPO production and stimulates erythropoiesis. It is currently being investigated as an oral treatment for anemia associated with CKD.
ln Vitro |
In PC12 cells, roxadustat (5-50 μM; 6 hours) dramatically reduces TBHP-induced apoptosis[2]. In PC12 cells, roxadustat (50 μM; 6 hours) stabilizes HIF-1α protein expression[2].
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ln Vivo |
Improved recovery from spinal cord injury and protection of motor neuron survival are two benefits of roxadustat (50 mg/kg; ip; daily for 7 days)[2].
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Cell Assay |
Apoptosis Analysis[2]
Cell Types: PC12 cells Tested Concentrations: 5, 20, 50 μM Incubation Duration: 6 hrs (hours) Experimental Results: Dramatically inhibited TBHP-induced apoptosis. Western Blot Analysis[2] Cell Types: PC12 cells Tested Concentrations: 50 μM Incubation Duration: 6 hrs (hours) Experimental Results: stabilized HIF-1α protein expression. |
Animal Protocol |
Animal/Disease Models: 12-week female C57BL/6 mice[2]
Doses: 50 mg/ kg Route of Administration: intraperitoneal (ip)injection; daily for 7 days Experimental Results: Protected the survival of motor neurons and improved recovery from spinal cord injury. |
References |
[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. |
Molecular Formula |
C19H16N2O5
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Molecular Weight |
352.34100
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CAS # |
808118-40-3
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Related CAS # |
Roxadustat-d5;2043026-13-5
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SMILES |
O=C(O)CNC(C1=C(O)C2=C(C(C)=N1)C=C(OC3=CC=CC=C3)C=C2)=O
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InChi Key |
YOZBGTLTNGAVFU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H16N2O5/c1-11-15-9-13(26-12-5-3-2-4-6-12)7-8-14(15)18(24)17(21-11)19(25)20-10-16(22)23/h2-9,24H,10H2,1H3,(H,20,25)(H,22,23)
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Chemical Name |
(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycine
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Synonyms |
Roxadustat; ASP1517; ASP 1517; ASP-1517; FG-4592; FG4592; FG-4592;
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~283.82 mM)
H2O : < 0.1 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.10 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5 mg/mL (14.19 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05970172 | Recruiting | Drug: Roxadustat | Chronic Kidney Disease Renal Anemia |
Astellas Pharma Global Development, Inc. |
January 16, 2024 | Phase 3 |
NCT04076943 | Completed Has Results |
Drug: Roxadustat | Chemotherapy Induced Anemia | FibroGen | August 20, 2019 | Phase 2 |
NCT06020833 | Not yet recruiting | Drug: Roxadustat in combination with retinoic acid |
Myelodysplastic Syndromes | Peking Union Medical College Hospital | August 2023 | Phase 1 Phase 2 |
NCT04454879 | Completed | Drug: Roxadustat | Renal Anemia | Peking University First Hospital | July 1, 2020 | Phase 4 |
Figure 1Study scheme. Abbreviations: IV, intravenous; pt, patient; TIW, thrice weekly. td> |
Figure 2Hemoglobin levels over time (6 weeks) by treatment group. (A) Hb levels over time by dose cohort for participants randomly assigned to 6 weeks of treatment in part 1. Hb level responders are defined as the number (percent) of patients whose Hb levels did not decrease by >0.5 g/dL from their baseline (primary efficacy end point in part 1). (B) Least squares mean Hb levels over time (19 weeks), roxadustat-treated versus epoetin alfa–treated patients. Closed diamonds are roxadustat (n = 61); open circles are epoetin alfa (n = 22). ∗P values are from Fisher exact test (2 sided) comparing roxadustat with epoetin alfa. Error bars signify standard error (SE) of the mean. td> |
Figure 3Baseline C-reactive protein (CRP) levels are correlated with (A) pre-enrollment epoetin alfa but not (B) roxadustat maintenance dose requirements. ∗N = 49: all participants randomly assigned to 19 weeks of roxadustat treatment and dosed beyond 12 weeks (maintenance phase) with valid baseline epoetin alfa dose data and valid baseline and average last 7 of 19 weeks of CRP data. Thus, this analysis did not include the 9 patients discontinued from roxadustat treatment for lack of efficacy (see Fig S1). Baseline CRP level was the average of the last 3 values prior to the first dose of study drug. CRP is plotted on the x-axis using a logarithmic scale. Abbreviation: LR, linear regression. td> |