Grouped product items

SKU

Size

Availability

Price

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

Synonyms	Roxadustat \| FG-4592 \| 808118-40-3 \| FG4592 \| Roxadustat (FG-4592) \| ASP1517 \| ASP 1517 \| N-[(4-Hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]glycine \| Roxadustat [USAN:INN] \| UNII-X3O30D9YMX \| X3O30D9YMX \| 2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]ac
Specifications & Purity	Moligand™, ≥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 Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Hypoxia-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

ALogP	3.4

Associated Targets(Human)

EGLN1 Tclin Egl nine homolog 1 (6 Activities)

Discover Target: EGLN1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EGLN2 Tclin Egl nine homolog 2 (0 Activities)

Discover Target: EGLN2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

F2 Tclin Thrombin (11687 Activities)

Discover Target: F2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ESR1 Tclin Estrogen receptor alpha (17718 Activities)

Discover Target: ESR1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PGR Tclin Progesterone receptor (8562 Activities)

Discover Target: PGR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)

Discover Target: CHRM2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 Activities)

Discover Target: HTR1A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)

Discover Target: ADRA2A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

AR Tclin Androgen Receptor (11781 Activities)

Discover Target: AR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

THRA Tclin Thyroid hormone receptor alpha (894 Activities)

Discover Target: THRA

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)

Discover Target: CHRM1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

GABRA1 Tclin GABA receptor alpha-1 subunit (399 Activities)

Discover Target: GABRA1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MAOA Tclin Monoamine oxidase A (11911 Activities)

Discover Target: MAOA

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

DRD1 Tclin Dopamine D1 receptor (9720 Activities)

Discover Target: DRD1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ACHE Tclin Acetylcholinesterase (18204 Activities)

Discover Target: ACHE

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PTGS1 Tclin Cyclooxygenase-1 (9233 Activities)

Discover Target: PTGS1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SLC6A2 Tclin Norepinephrine transporter (10102 Activities)

Discover Target: SLC6A2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SLC6A4 Tclin Serotonin transporter (12625 Activities)

Discover Target: SLC6A4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ADRA1A Tclin Alpha-1a adrenergic receptor (8359 Activities)

Discover Target: ADRA1A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

OPRM1 Tclin Mu opioid receptor (19785 Activities)

Discover Target: OPRM1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

DRD3 Tclin Dopamine D3 receptor (14368 Activities)

Discover Target: DRD3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SLC6A3 Tclin Dopamine transporter (10535 Activities)

Discover Target: SLC6A3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PDE3A Tclin Phosphodiesterase 3A (3309 Activities)

Discover Target: PDE3A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 Activities)

Discover Target: HTR2B

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

TBXA2R Tclin Thromboxane A2 receptor (5717 Activities)

Discover Target: TBXA2R

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

THRB Tclin Thyroid hormone receptor beta-1 (7926 Activities)

Discover Target: THRB

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PDE4A Tclin Phosphodiesterase 4A (1943 Activities)

Discover Target: PDE4A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ADORA3 Tchem Adenosine A3 receptor (15931 Activities)

Discover Target: ADORA3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HRH3 Tclin Histamine H3 receptor (10389 Activities)

Discover Target: HRH3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

AOX1 Tchem Aldehyde oxidase (429 Activities)

Discover Target: AOX1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Homo sapiens (32628 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HEK293 (82097 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HUVEC (11049 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HIF1A Tchem Hypoxia-inducible factor 1 alpha (6027 Activities)

Discover Target: HIF1A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

EGLN1 Tclin Egl nine homolog 1 (1702 Activities)

Discover Target: EGLN1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

EGLN3 Tclin Egl nine homolog 3 (250 Activities)

Discover Target: EGLN3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HIF1AN Tbio Hypoxia-inducible factor 1-alpha inhibitor (79 Activities)

Discover Target: HIF1AN

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

EPAS1 Tclin Endothelial PAS domain-containing protein 1 (498 Activities)

Discover Target: EPAS1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

FTO Tchem Alpha-ketoglutarate-dependent dioxygenase FTO (473 Activities)

Discover Target: FTO

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HK-2 (249 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Hep 3B2 (2332 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

L02 (4864 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

OGFOD1 Tbio Prolyl 3-hydroxylase OGFOD1 (5 Activities)

Discover Target: OGFOD1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SARS-CoV-2 (38078 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

A085R Prolyl 4-hydroxylase (72 Activities)

Discover Target: A085R

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

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

Database links

PubChem CID	11256664
CAS Registry No.	808118-40-3
ChEMBL Ligand	CHEMBL2338329
RCSB PDB Ligand	8HO
DrugCentral Ligand	5371

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

13 results found

Lot Number	Certificate Type	Date	Item
K2116151	Certificate of Analysis	Sep 13, 2023	F126178
K2116152	Certificate of Analysis	Sep 13, 2023	F126178
H1507110	Certificate of Analysis	Mar 16, 2023	F126178
B2311525	Certificate of Analysis	Nov 25, 2022	F126178
B2311528	Certificate of Analysis	Nov 25, 2022	F126178
B2311535	Certificate of Analysis	Nov 25, 2022	F126178
B2311537	Certificate of Analysis	Nov 25, 2022	F126178
B2311546	Certificate of Analysis	Nov 25, 2022	F126178
B2311547	Certificate of Analysis	Nov 25, 2022	F126178
B2311548	Certificate of Analysis	Nov 25, 2022	F126178
B2311579	Certificate of Analysis	Nov 25, 2022	F126178
L1827045	Certificate of Analysis	Sep 17, 2022	F126178
L1827046	Certificate of Analysis	Sep 17, 2022	F126178

Chemical and Physical Properties

Solubility	DMSO >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.

Alternative Products

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]

References

1. Bouchie A. (2013) First-in-class anemia drug takes aim at Amgen's dominion.. Nat Biotechnol, 31 (11): (948-9). [PMID:24213751]
2. Forristal CE, Levesque JP. (2014) Targeting the hypoxia-sensing pathway in clinical hematology.. Stem Cells Transl Med, 3 (2): (135-40). [PMID:24371328]
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]

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

Basic Description

Product Properties

Associated Targets(Human)

Associated Targets(non-human)

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

more

Chemical and Physical Properties

Safety and Hazards(GHS)

Related Documents

Alternative Products

Citations of This Product

References

Solution Calculators

Molarity Calculator

Dilution Calculator

Reconstitution Calculator