Roxadustat (FG-4592)

Alias: Roxadustat; ASP1517; ASP 1517; ASP-1517; FG-4592; FG4592; FG-4592;

Cat No.:V0293 Purity: ≥98%

COA Product Data Instructions for use SDS

Roxadustat (FG-4592) Chemical Structure CAS No.: 808118-40-3
Product category: HIF

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Roxadustat (FG-4592):

Roxadustat-d5

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

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.

Biological Activity I Assay Protocols (From Reference)

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].
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].
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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C19H16N2O5
Molecular Weight	352.34100
CAS #	808118-40-3
Related CAS #	Roxadustat-d5;2043026-13-5
SMILES	O=C(O)CNC(C1=C(O)C2=C(C(C)=N1)C=C(OC3=CC=CC=C3)C=C2)=O
InChi Key	YOZBGTLTNGAVFU-UHFFFAOYSA-N
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)
Chemical Name	(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycine
Synonyms	Roxadustat; ASP1517; ASP 1517; ASP-1517; FG-4592; FG4592; FG-4592;
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)

Solubility Data

Solubility (In Vitro)	DMSO : ≥ 100 mg/mL (~283.82 mM) H2O : < 0.1 mg/mL
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. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a 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. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO : ≥ 100 mg/mL (~283.82 mM)
H2O : < 0.1 mg/mL

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.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a 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.

(Please use freshly prepared in vivo formulations for optimal results.)

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.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

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Concentration (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

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g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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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.

Note： (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.

Clinical Trial Information

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

Biological Data

Figure 1Study scheme. Abbreviations: IV, intravenous; pt, patient; TIW, thrice weekly.

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.

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.