FG-4592 - ≥98%, high purity , Hypoxia-inducible factor prolyl hydroxylase inhibitor, CAS No.808118-40-3, Hypoxia-inducible factor prolyl hydroxylase inhibitor

Item Number
F126178
Grouped product items
SKUSizeAvailabilityPrice Qty
F126178-10mg
10mg
In stock
$58.90
F126178-50mg
50mg
In stock
$105.90
F126178-250mg
250mg
In stock
$225.90
F126178-500mg
500mg
In stock
$343.90

Basic Description

SynonymsFG-4592 (ASP1517) | NCGC00346527-01 | NCGC00346527-07 | N-[(4-hydroxy-1-methyl-7-phenoxyisoquinolin-3-yl)carbonyl]glycine | Roxadustat | YOZBGTLTNGAVFU-UHFFFAOYSA-N | 2-(4-hydroxy-1-Methyl-7-phenoxyisoquinoline-3-carboxaMido)acetic acid | Evrenzo | J-5227
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological Mechanisms

FG-4592 is an inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase currently in clinical development for the treatment of anemia. FG-4592 stabilizes the activities of HIF, a cytosolic transcription factor, leading to activation

Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionHypoxia-inducible factor prolyl hydroxylase inhibitor
Product Description

FG-4592 is an HIF α prolyl hydroxylase inhibitor, stabilizes HIF-2 and induces EPO production.

Product Properties

ALogP3.4

Associated Targets(Human)

EGLN1 Tclin Egl nine homolog 1 (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EGLN2 Tclin Egl nine homolog 2 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
F2 Tclin Thrombin (11687 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ESR1 Tclin Estrogen receptor alpha (17718 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PGR Tclin Progesterone receptor (8562 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AR Tclin Androgen Receptor (11781 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
THRA Tclin Thyroid hormone receptor alpha (894 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TBXA2R Tclin Thromboxane A2 receptor (5717 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
THRB Tclin Thyroid hormone receptor beta-1 (7926 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PDE4A Tclin Phosphodiesterase 4A (1943 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AOX1 Tchem Aldehyde oxidase (429 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Homo sapiens (32628 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK293 (82097 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HUVEC (11049 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HIF1A Tchem Hypoxia-inducible factor 1 alpha (6027 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EGLN1 Tclin Egl nine homolog 1 (1702 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EGLN3 Tclin Egl nine homolog 3 (250 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HIF1AN Tbio Hypoxia-inducible factor 1-alpha inhibitor (79 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EPAS1 Tclin Endothelial PAS domain-containing protein 1 (498 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FTO Tchem Alpha-ketoglutarate-dependent dioxygenase FTO (473 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HK-2 (249 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hep 3B2 (2332 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
L02 (4864 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
A085R Prolyl 4-hydroxylase (72 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]acetic acid
INCHI 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)
InChi Key YOZBGTLTNGAVFU-UHFFFAOYSA-N
Canonical SMILES CC1=C2C=C(C=CC2=C(C(=N1)C(=O)NCC(=O)O)O)OC3=CC=CC=C3
Isomeric SMILES CC1=C2C=C(C=CC2=C(C(=N1)C(=O)NCC(=O)O)O)OC3=CC=CC=C3
PubChem CID 11256664
Molecular Weight 352.34

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

13 results found

Lot NumberCertificate TypeDateItem
B2311535Certificate of AnalysisNov 18, 2024 F126178
B2311537Certificate of AnalysisNov 18, 2024 F126178
B2311546Certificate of AnalysisNov 18, 2024 F126178
B2311548Certificate of AnalysisNov 18, 2024 F126178
B2311579Certificate of AnalysisNov 18, 2024 F126178
B2311547Certificate of AnalysisNov 06, 2024 F126178
B2311528Certificate of AnalysisNov 06, 2024 F126178
B2311525Certificate of AnalysisNov 06, 2024 F126178
K2116151Certificate of AnalysisSep 13, 2023 F126178
K2116152Certificate of AnalysisSep 13, 2023 F126178
H1507110Certificate of AnalysisMar 16, 2023 F126178
L1827045Certificate of AnalysisSep 17, 2022 F126178
L1827046Certificate of AnalysisSep 17, 2022 F126178

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Chemical and Physical Properties

SolubilityDMSO >70 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H335:May cause respiratory irritation

H302:Harmful if swallowed

H332:Harmful if inhaled

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352:IF ON SKIN: wash with plenty of water.

P321:Specific treatment (see ... on this label).

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P271:Use only outdoors or in a well-ventilated area.

P270:Do not eat, drink or smoke when using this product.

P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing.

P403+P233:Store in a well-ventilated place. Keep container tightly closed.

P362+P364:Take off contaminated clothing and wash it before reuse.

P330:Rinse mouth.

P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes.

P301+P317:IF SWALLOWED: Get medical help.

P317:Get emergency medical help.

P337+P317:If eye irritation persists: Get medical help.

P332+P317:If skin irritation occurs: Get medical help.

P319:Get medical help if you feel unwell.

Related Documents

Citations of This Product

1. Yujing Wang, Min Xiao, Feng Cai, Yang Li, Tianli Shi, Xiaoyan Zhou, Shuhong Tian, Denggao Huang.  (2023)  Roxadustat ameliorates vascular calcification in CKD rats by regulating HIF-2α/HIF-1α.  ENVIRONMENTAL TOXICOLOGY,      [PMID:38156404] [10.1002/tox.24116]

References

1. Bouchie A.  (2013)  First-in-class anemia drug takes aim at Amgen's dominion..  Nat Biotechnol,  31  (11): (948-9).  [PMID:24213751] [10.1021/op500134e]
2. Forristal CE, Levesque JP.  (2014)  Targeting the hypoxia-sensing pathway in clinical hematology..  Stem Cells Transl Med,  (2): (135-40).  [PMID:24371328] [10.1021/op500134e]
3. Yujing Wang, Min Xiao, Feng Cai, Yang Li, Tianli Shi, Xiaoyan Zhou, Shuhong Tian, Denggao Huang.  (2023)  Roxadustat ameliorates vascular calcification in CKD rats by regulating HIF-2α/HIF-1α.  ENVIRONMENTAL TOXICOLOGY,      [PMID:38156404] [10.1002/tox.24116]

Solution Calculators