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
SMILES
OC(=O)CNC(=O)C1=C(O)C2=C(C=CC=C2)C(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)
Molecular Formula | C12H9ClN2O4 |
Molecular Weight | 280.664 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/24894560Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/23234607 | https://www.ncbi.nlm.nih.gov/pubmed/23547775 | https://www.ncbi.nlm.nih.gov/pubmed/21115615
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24894560
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/23234607 | https://www.ncbi.nlm.nih.gov/pubmed/23547775 | https://www.ncbi.nlm.nih.gov/pubmed/21115615
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 Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5697 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23234607 |
3.9 µM [IC50] | ||
Target ID: CHEMBL2331065 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23547775 |
2.8 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21115615
20 mg/kg for 7 days.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24894560
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
Created
by
admin
on
Edited
Fri Dec 15 21:13:29 UTC 2023
by
admin
on
Fri Dec 15 21:13:29 UTC 2023
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Record UNII |
RU921DS4Z5
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Record Status |
Validated (UNII)
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Record Version |
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6914666
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223387-75-5
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RU921DS4Z5
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admin on Fri Dec 15 21:13:29 UTC 2023 , Edited by admin on Fri Dec 15 21:13:29 UTC 2023
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