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Details

Stereochemistry ACHIRAL
Molecular Formula C12H9ClN2O4
Molecular Weight 280.664
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FG-2216

SMILES

OC(=O)CNC(=O)C1=C(O)C2=CC=CC=C2C(Cl)=N1

InChI

InChIKey=OUQVKRKGTAUJQA-UHFFFAOYSA-N
InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17)

HIDE SMILES / InChI

Molecular Formula C12H9ClN2O4
Molecular Weight 280.664
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

FG 2216 is an erythropoietic small molecule prolyl hydroxylase inhibitor, originally developed by FibroGen, that is undergoing development for the treatment of anemia. PDH inhibitor FG-2216 was orally bioavailable and induced significant and reversible EPO induction in vivo. Chronic oral dosing in male rhesus macaques was well tolerated, significantly increased erythropoiesis, and prevented anemia induced by weekly phlebotomy. Furthermore, modest increases in HbF-containing red cells and reticulocytes were demonstrated by flow cytometry. FG 2216 had been in phase II clinical trials for the treatment of anemia, however, all researchers on this drug candidate were discontinued.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
3.9 µM [IC50]
2.8 µM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
179 μg/mL
20 mg/kg single, oral
FG-2216 plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
3660 μg × h/mL
20 mg/kg single, oral
FG-2216 plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
15.7 h
20 mg/kg single, oral
FG-2216 plasma
Homo sapiens

Doses

PubMed

Sample Use Guides

In Vivo Use Guide
20 mg/kg for 7 days.
Route of Administration: Oral
In Vitro Use Guide
Hep3B cells were used for activity evaluation. Cells were treated with FG 2216 (50 and 100mkM) for 24h. EPO expression due to PHD2 inhibition was determined using the EPO ELISA method
Substance Class Chemical
Record UNII
RU921DS4Z5
Record Status Validated (UNII)
Record Version