FG-4592 Roxadustat powder CAS 808118-40-3 high purity HIF prolyl hydroxylase inhibitor for biomedical research

CAS 808118-40-3 FG4592 Roxadustat Powder HIF Prolyl Hydroxylase Inhibitor for Renal Anemia Research

Premium 99% FG4592 Roxadustat crystalline powder CAS 808118-40-3, potent oral HIF-PH inhibitor. Ideal for renal anemia, kidney protection and hypoxia signaling pathway pharmacological research.
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FG-4592 / Roxadustat (CAS 808118-40-3) HIF-PH Inhibitor | Stabilizes HIF-1α/2α, Erythropoiesis & Anemia Research Compound

FG-4592 (Roxadustat) CAS 808118-40-3
HIF Prolyl-Hydroxylase (HIF-PH / PHD) Inhibitor — Anemia & Hypoxia Research

FG-4592 (roxadustat; CAS 808118-40-3) is a potent, orally active hypoxia-inducible factor prolyl-hydroxylase (HIF-PH / PHD) inhibitor that stabilizes HIF-1α/2α (PHD2 IC50 ~1.7 µM; Ki ~20 nM vs α-KG) and stimulates erythropoietin. Molecular formula C19H16N2O5, MW 352.34. Research-grade with COA.

HIF-PH Inhibitor FG-4592 Roxadustat PHD Inhibitor Hypoxia Anemia Erythropoietin HIF Stabilizer
Request a Quote Technical Specs
352.34
MW (C19H16N2O5)
~1.7 µM
PHD2 IC50
HIF
Stabilizes HIF-1α/2α

Molecular Information

Name: FG-4592 (Roxadustat)
CAS: 808118-40-3
Formula: C19H16N2O5
MW: 352.34 g/mol
Class: 4-Hydroxyisoquinoline glycinamide
Core: 4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamide glycine conjugate
Target: HIF prolyl-hydroxylase (PHD1/2/3)
IC50: PHD2 ~1.7 µM
Appearance: White to beige powder
Synonyms: Roxadustat / ASP1517
Storage: -20 C
🧪
CAS Number
808118-40-3
⚖️
Molecular Weight
352.34
🎯
Primary Activity
HIF-PH Inhibitor
✅
Purity
≥98%

Product Technical Specifications

Complete physicochemical properties and QC parameters for FG-4592 (Roxadustat) (CAS 808118-40-3)

📋 Physicochemical Properties

  • Product NameFG-4592 (Roxadustat)
  • IUPAC Core2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]acetic acid
  • CAS Number808118-40-3
  • SynonymsRoxadustat; ASP1517; AZD9941; FG4592
  • Molecular FormulaC19H16N2O5
  • Molecular Weight352.34 g/mol
  • SourceSynthetic small molecule (FibroGen / Astellas / AstraZeneca)
  • AppearanceWhite to beige powder
  • Melting PointNot reported
  • Water SolubilityLow
  • Organic SolubilityDMSO ~17-46 mg/mL; ethanol (warmed)
  • Compound Class4-Hydroxyisoquinoline HIF-PH inhibitor
  • HS Code2934.99

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormSolid powder
  • Primary TargetHIF prolyl-hydroxylase (PHD1/2/3 / EGLN1-3)
  • Pathway ReadoutStabilized HIF-1α/2α; ↑ EPO, VEGF; ↓ hepcidin
  • SelectivityHIF-PH vs FIH (>150 µM); α-KG-competitive
  • Storage Condition-20 C, sealed, protect from light
  • Solution StabilityAliquot DMSO stocks; avoid freeze-thaw
  • ShippingBlue ice / cold chain recommended
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes1g / 5g / 10g / 100g / 1KG
  • Stock StatusIn Stock
  • Use StatementResearch use only; not for human/clinical use

Key Molecular Targets & Pathway Nodes

FG-4592 targets the HIF prolyl-hydroxylases (PHD1/2/3, also EGLN1-3) that normally mark HIF-α for destruction; inhibition stabilizes HIF and re-activates the hypoxia response.

🧬 PHD1 (EGLN2) 🧬 PHD2 (EGLN1) 🧬 PHD3 (EGLN3) 🧬 HIF-1α / HIF-2α 🧱 VHL / Ubiquitin Proteasome 🧱 pVHL Recognition 🩸 Erythropoietin (EPO) 🩸 Iron Metabolism / Hepcidin 🔗 VEGF / Angiogenesis 🔗 Glycolysis Genes 🧪 Hypoxia Response ⚡ α-Ketoglutarate (substrate)

How FG-4592 Works: Stabilizing HIF by Inhibiting its 'Oxygen Sensor'

FG-4592 competitively blocks HIF prolyl-hydroxylase (PHD), so HIF-α escapes degradation and switches on the hypoxia-response program

1

α-KG-Competitive PHD Inhibition

Under normoxia, PHD enzymes use O2 and α-ketoglutarate (α-KG) to hydroxylate HIF-α, marking it for VHL-mediated degradation. FG-4592 is α-KG-competitive (Ki ~20 nM) and blocks PHD1/2/3 (PHD2 IC50 ~1.7 µM), preventing this hydroxylation.

2

HIF-α Stabilization

With hydroxylation blocked, HIF-1α and HIF-2α are no longer recognized by VHL and are stabilized, accumulating in the nucleus to form active HIF transcription complexes.

3

Hypoxia-Response Program: EPO, Iron & Angiogenesis

Stabilized HIF drives erythropoietin (EPO) production, improves iron metabolism (lowering hepcidin) and induces VEGF and glycolytic genes. This is the basis of anemia and ischemia/hypoxia research using FG-4592.

⚖️ FG-4592 vs Other HIF-PH Inhibitors

  • FG-4592 / Roxadustat (this product)PHD1/2/3 inhibitor; Ki ~20 nM vs α-KG; PHD2 IC50 ~1.7 µM
  • Deferoxamine (DFO)Iron chelator; indirect HIF stabilizer
  • CoCl2Prolyl-hydroxylase inhibitor (metal-based)
  • Shared PathwayHIF stabilization / hypoxia response
  • Key DistinctionSelective PHD vs FIH (>150 µM)
  • OutputEPO ↑, hepcidin ↓, VEGF ↑

♻️ Downstream Biological Consequences

  • EnzymePHD1/2/3 blocked (α-KG-competitive)
  • FactorHIF-1α / HIF-2α stabilized
  • HematologyEPO ↑; erythropoiesis ↑
  • IronHepcidin ↓; iron availability ↑
  • VasculatureVEGF ↑; angiogenesis
  • MetabolismGlycolysis genes ↑ (pseudo-hypoxia)

Research Applications & Models

A central tool for probing oxygen sensing, with direct relevance to anemia, ischemia and iron metabolism.

🩸

Anemia & Erythropoiesis Models

The flagship use: FG-4592 stabilizes HIF to induce EPO and stimulate red-cell production; benchmarked in CKD-anemia and hypoxia models.

HIF / EPO
🫁

Hypoxia & Ischemia Research

Used to mimic and study the hypoxia response, tissue adaptation and ischemic preconditioning.

Hypoxia response
🩸

Iron Metabolism & Hepcidin

Investigated for lowering hepcidin and improving iron availability in anemia-of-inflammation models.

Iron / Hepcidin
🔬

HIF / PHD Biology

A fiducial α-KG-competitive PHD inhibitor for hydroxylases, VHL recognition and HIF stability assays.

HIF-PHD
🩸

Angiogenesis

Studied for VEGF induction and vessel formation in regenerative contexts.

VEGF / Angio
⚖️

Oxygen-Sensing Panel

Benchmarked against DFO and CoCl2 to separate direct PHD inhibition from indirect stabilizers.

Oxygen panel

Key Literature & Landmark Publications

The nonclinical pharmacology and clinical development of roxadustat (FG-4592).

Provenzano R, et al. Roxadustat (FG-4592) for the treatment of anemia in chronic kidney disease. Clin J Am Soc Nephrol. 2016;11(6):982-91.
doi: 10.2215/CJN.13061215
Besarab A, et al. Roxadustat for anemia in patients with end-stage renal disease undergoing hemodialysis. J Am Soc Nephrol. 2016;27(4):1225-33.
doi: 10.1681/ASN.2015040430
Jain IH, et al. Genetics of PHDs in mitochondrial function & HIF. Science. 2016;352(6281):54-61.
doi: 10.1126/science.aac4858
Nonclinical characterization: roxadustat inhibits PHD1/2/3 (IC50 1.04/1.74/0.36 µM); FIH IC50 >150 µM.
Landmark reference
Wu Y, et al. Medicinal chemistry of HIF-PH inhibitors (roxadustat class). J Med Chem. 2018;61(12):5332-49.
doi: 10.1021/acs.jmedchem.7b01184

Available Sizes & Ordering

Research-grade FG-4592 / Roxadustat (CAS 808118-40-3) with full QC documentation; standard packs and bulk custom quantities supported.

TierPack SizeStock StatusSuitable ForLead Time
Standard1gIn StockHIF-PHD & EPO assaysCold chain
Medium5gIn StockHypoxia, anemia & iron modelsCold chain
Large10gIn StockLong-term in vivo & formulation studiesCold chain
Bulk100gIn StockFormulation & process developmentQuote to confirm
Industrial1KGMade to orderPilot/production scale, CMO supplyBatch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is FG-4592 (roxadustat) and what does it do?
FG-4592, also called roxadustat (CAS 808118-40-3), is a potent, orally active HIF prolyl-hydroxylase (HIF-PH / PHD) inhibitor. It competitively blocks PHD1/2/3 (PHD2 IC50 ~1.7 µM; Ki ~20 nM vs α-ketoglutarate), stabilizing HIF-1α/2α and inducing erythropoietin. Formula C19H16N2O5, MW 352.34.
How is FG-4592 different from deferoxamine or cobalt chloride?
DFO is an iron chelator that stabilizes HIF indirectly; CoCl2 is a metal-based nonspecific PHD inhibitor. FG-4592 is a direct, selective α-KG-competitive PHD inhibitor (selective vs FIH, IC50 >150 µM), giving a cleaner, more defined HIF-stabilization phenotype.
What is the mechanism in anemia research?
PHD enzymes normally hydroxylate HIF-α so it is degraded. FG-4592 blocks this, so HIF accumulates and switches on the hypoxia program: erythropoietin (EPO) rises, hepcidin falls (improving iron availability) and red-cell production increases — the basis of CKD-anemia and erythropoiesis research.
What are the key experimental readouts?
Readouts include HIF-1α/2α protein stabilization (Western), EPO by ELISA, hepcidin, VEGF, hypoxia-response-reporter activity, and PHD hydroxyltransferase assays (Ki vs α-KG).
How soluble is FG-4592 and how prepared?
FG-4592 is soluble in DMSO (~17-46 mg/mL) and ethanol (with warming); aqueous solubility is low. For cell assays dilute DMSO stock into medium (final DMSO <=0.1% v/v); for in vivo use validated vehicles/suspensions. Store the solid at -20 C, desiccated and protected from light; aliquot stocks.
Is QC documentation provided?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity, structural confirmation and MS data. MSDS/SDS and Certificates of Origin are available on request. Sample evaluation is available for qualified institutions — please contact us.

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Research-grade FG-4592 / Roxadustat (CAS 808118-40-3) — purity ≥98% HPLC, COA included
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