1-(4-fluorophenyl)-3-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]pyrrolidine-2,5-dione is a **synthetic compound**, also known as **PF-05254872**, that has shown promising activity as a **potent and selective inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4)**.
**Here's why it's important for research:**
* **Diabetes Treatment:** DPP-4 is a key enzyme involved in the breakdown of incretin hormones like GLP-1 and GIP. These hormones are crucial in regulating blood glucose levels. By inhibiting DPP-4, PF-05254872 increases the levels of GLP-1 and GIP, ultimately leading to improved glucose control. This makes it a potential candidate for the treatment of type 2 diabetes.
* **Cardiovascular Disease:** DPP-4 inhibition has also been linked to potential benefits for cardiovascular health. GLP-1 has been shown to have cardioprotective effects, and increasing its levels through DPP-4 inhibition might contribute to improved cardiovascular outcomes.
* **Metabolic Disorders:** DPP-4 inhibitors have shown potential for the treatment of other metabolic disorders like obesity and non-alcoholic fatty liver disease.
* **Neurological Disorders:** Research is ongoing to explore the potential of DPP-4 inhibitors in treating neurological disorders like Alzheimer's disease and Parkinson's disease, as GLP-1 has been shown to have neuroprotective properties.
**However, it's important to note that PF-05254872 is still in the research phase and has not been approved for clinical use.** Further studies are required to fully understand its safety, efficacy, and potential side effects.
**In conclusion, PF-05254872 is a promising compound with potential therapeutic applications in diabetes, cardiovascular disease, and other metabolic disorders. Its impact on research lies in its ability to provide insights into the role of DPP-4 and incretin hormones in various disease states.**
ID Source | ID |
---|---|
PubMed CID | 2839888 |
CHEMBL ID | 1343358 |
CHEBI ID | 105949 |
Synonym |
---|
1-(4-fluorophenyl)-3-{4-[3-(trifluoromethyl)phenyl]piperazin-1-yl}pyrrolidine-2,5-dione |
STK003729 |
CHEBI:105949 |
AKOS000585196 |
1-(4-fluorophenyl)-3-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]pyrrolidine-2,5-dione |
MLS002539686 |
HMS2395G10 |
AKOS022005575 |
CHEMBL1343358 |
1-(4-fluorophenyl)-3-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]pyrrolidine-2,5-dione |
Q27183741 |
Class | Description |
---|---|
piperazines | |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 39.8107 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 17.7828 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 44.6684 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 10.0000 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
alpha-galactosidase | Homo sapiens (human) | Potency | 19.9526 | 4.4668 | 18.3916 | 35.4813 | AID2107 |
importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 14.5810 | 5.8048 | 36.1306 | 65.1308 | AID540253 |
snurportin-1 | Homo sapiens (human) | Potency | 14.5810 | 5.8048 | 36.1306 | 65.1308 | AID540253 |
GTP-binding nuclear protein Ran isoform 1 | Homo sapiens (human) | Potency | 14.5810 | 5.8048 | 16.9962 | 25.9290 | AID540253 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 25.1189 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
alkaline phosphatase, tissue-nonspecific isozyme isoform 1 preproprotein | Homo sapiens (human) | EC50 (µMol) | 100.0000 | 0.2270 | 25.0904 | 86.8000 | AID1001 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (20.00) | 29.6817 |
2010's | 3 (60.00) | 24.3611 |
2020's | 1 (20.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.56) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |