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FG-4592 (ASP1517)HIF prolyl-hydroxylase inhibitor

FG-4592 (ASP1517)

Catalog No. A4187
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
Evaluation Sample $28.00 In stock
10mg $50.00 In stock
50mg $170.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

FG-4592 (ASP1517)

Biological Activity

Description FG-4592 is an inhibitor of HIF α prolyl hydroxylase.
Targets HIF α prolyl hydroxylase          
IC50            

Protocol

Cell experiment [1]:

Cell lines

PC-12 cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reacting condition

5, 20 or 50 μM

Applications

FG-4592 showed significant protection effect against the TBHP-induced cell death.

Animal experiment [1]:

Animal models

Mouse model of spinal cord injury

Dosage form

50mg/kg/day; i.p.; for 7 days

Applications

In a mouse model of spinal cord injury, FG-4592 administration improved recovery and increased the survival of neurons in spinal cord lesions.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Wu K, Zhou K, Wang Y, Zhou Y, Tian N, Wu Y, Chen D, Zhang D, Wang X, Xu H, Zhang X. 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.

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Chemical Properties

Cas No. 808118-40-3 SDF Download SDF
Chemical Name 2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]acetic acid
Canonical SMILES CC1=NC(=C(C2=C1C=C(C=C2)OC3=CC=CC=C3)O)C(=O)NCC(=O)O
Formula C19H16N2O5 M.Wt 352.34
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

FG-4592 (also known as ASP1517), 2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid, is a potent small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH), an enzyme up-regulating the expression of endogenous human erythropoietin (Epo). It is currently being investigated as an oral treatment for anemia associated with chronic kidney disease (CKD). Unlike other anemia treating agents, erythropoiesis-stimulating agents (ESAs), FG-4592 inhibits HIF, through a distinctive mechanism, by stabilization of HIF. According to previous studies, FG-4592 is capable of correcting and maintaining hemoglobin levels in CKD patients not receiving dialysis and in patients of end-stage renal disease who receives dialysis but do not need intravenous iron supplement.

Reference

1. Luis Borges. Different modalities of erythropoiesis stimulating agents. Port J Nephrol Hypert 2010; 24(2): 137-145
2. “FibroGen and Astellas announce initiation of phase 3 trial of FG-4592/ASP1517 for treatment of anemia of chronic kidney disease” Fibrogen Press Release. Dec 11 2012
3. “FibroGen announces initiation of phase 2b studies of FG-4592, an oral HIF prolyl hydroxylase inhibitor, for treatment of anemia”