2-(3-chlorophenyl)-5-(prop-2-enylamino)-4-oxazolecarbonitrile, also known as **GW842507X**, is 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 degradation of incretin hormones, like GLP-1 and GIP, which play a crucial role in regulating blood glucose levels. Inhibiting DPP-4 allows these incretins to persist in the bloodstream for longer, leading to increased insulin secretion and improved glucose control. This makes GW842507X a promising candidate for the treatment of type 2 diabetes.
* **Metabolic Disorders:** DPP-4 inhibition has also been linked to benefits in other metabolic disorders, such as obesity and cardiovascular disease.
* **Drug Development:** GW842507X has served as a valuable tool in understanding the role of DPP-4 in various physiological processes. Its high selectivity and potency have made it a useful model compound for the development of novel DPP-4 inhibitors with improved therapeutic properties.
* **Research into DPP-4:** GW842507X's ability to inhibit DPP-4 has allowed researchers to study the enzyme's function in more detail and explore its potential involvement in other biological processes.
**It's important to note that:**
* While GW842507X holds promise as a potential drug, it is not currently commercially available.
* Further research is ongoing to evaluate its safety and efficacy in humans.
Overall, 2-(3-chlorophenyl)-5-(prop-2-enylamino)-4-oxazolecarbonitrile (GW842507X) is a significant research tool that has contributed to our understanding of DPP-4 and its potential as a target for drug development. It is a potent and selective inhibitor of DPP-4, which makes it valuable for studying the role of this enzyme in various metabolic disorders and for developing new treatments for diabetes and other related conditions.
ID Source | ID |
---|---|
PubMed CID | 2218783 |
CHEMBL ID | 1551144 |
CHEBI ID | 92521 |
Synonym |
---|
NCGC00183415-01 |
MLS002276476 |
smr001318014 |
STK896026 |
2-(3-chlorophenyl)-5-(prop-2-en-1-ylamino)-1,3-oxazole-4-carbonitrile |
2-(3-chlorophenyl)-5-(prop-2-enylamino)-1,3-oxazole-4-carbonitrile |
HMS2215E04 |
AKOS005636253 |
HMS3329D13 |
CHEMBL1551144 |
CHEBI:92521 |
SR-01000284442-1 |
sr-01000284442 |
Q27164251 |
2-(3-chlorophenyl)-5-(prop-2-enylamino)-4-oxazolecarbonitrile |
Class | Description |
---|---|
1,3-oxazoles | |
[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) |
---|---|---|---|---|---|---|---|
ATAD5 protein, partial | Homo sapiens (human) | Potency | 23.0999 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
Smad3 | Homo sapiens (human) | Potency | 35.4813 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 89.1251 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 50.1187 | 3.5481 | 19.5427 | 44.6684 | AID743266 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 70.7946 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 7.0795 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
plasminogen precursor | Mus musculus (house mouse) | Potency | 7.0795 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 7.0795 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
geminin | Homo sapiens (human) | Potency | 29.0929 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 24.6433 | 0.0601 | 10.7453 | 37.9330 | AID485367; AID504636; AID504637 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
[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] |