Details
Stereochemistry | ACHIRAL |
Molecular Formula | C23H27N5O2 |
Molecular Weight | 405.4928 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)N1N=CC2=C1C(=O)CC3(CCN(CC3)C(=O)C4=CC=C5N=C(C)NC5=C4)C2
InChI
InChIKey=BDXXSFOJPYSYOC-UHFFFAOYSA-N
InChI=1S/C23H27N5O2/c1-14(2)28-21-17(13-24-28)11-23(12-20(21)29)6-8-27(9-7-23)22(30)16-4-5-18-19(10-16)26-15(3)25-18/h4-5,10,13-14H,6-9,11-12H2,1-3H3,(H,25,26)
PF-05175157 exhibited good potencies against the two isoforms of the Acetyl-CoA carboxylase enzyme (ACC1 and ACC2) from human and rat. PF-05175157 has undergone multiple clinical trials in healthy volunteers and for the treatment of diabetes mellitus. PF-05175157 was in the phase II when the development was discontinued due to safety concerns. Among potential barriers for the use of ACC inhibitors in humans include concerns of increased risk of myocardial injury following an ischemic event. PF-05175157 reduced the multiplication of West Nile virus (WNV), dengue virus (DENV), and Zika virus (ZIKV) in cultured cells, which is compatible with the predicted broad spectrum of host targeting antivirals. PF-05175157 reduced the peak of viremia in WNV-infected mice, supporting that ACC is a valuable target for antiviral intervention. PF05175157 also reduced the viral burden in the kidney of infected mice.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2397 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25423286 |
27.0 nM [IC50] | ||
Target ID: CHEMBL4829 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25423286 |
33.0 nM [IC50] |
PubMed
Title | Date | PubMed |
---|---|---|
Synthesis, Biological Evaluation and Molecular Docking Studies of Piperidinylpiperidines and Spirochromanones Possessing Quinoline Moieties as Acetyl-CoA Carboxylase Inhibitors. | 2015 Sep 7 |
|
Discontinued drug therapies to treat diabetes in 2015. | 2017 Feb |
|
Targeting host metabolism by inhibition of acetyl-Coenzyme A carboxylase reduces flavivirus infection in mouse models. | 2019 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/30999821
Curator's Comment: Mice data
20 mg/kg twice a day
Route of Administration:
Oral
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P826WR56FI
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1301214-47-0
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300000041355
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ACTIVE MOIETY