1-(3-chloro-4-methoxyphenyl)sulfonyl-N-(3-pyridinyl)-3-piperidinecarboxamide, also known as **MK-0677**, is a selective and potent **agonist of the growth hormone secretagogue receptor (GHS-R)**. This means that it binds to and activates the GHS-R, leading to the release of growth hormone (GH).
**Why is it important for research?**
* **Growth hormone deficiency:** MK-0677 is being investigated as a potential treatment for growth hormone deficiency (GHD) in adults. GHD is a condition characterized by low levels of GH, which can lead to various health problems, including fatigue, decreased muscle mass, and increased body fat.
* **Metabolic disorders:** Studies have shown that MK-0677 may have beneficial effects on metabolic disorders such as obesity, diabetes, and fatty liver disease. It has been shown to increase insulin sensitivity, reduce body weight, and improve lipid profiles.
* **Muscle growth and performance:** MK-0677 has been investigated for its potential to enhance muscle growth and performance in athletes. It has been shown to increase muscle protein synthesis and decrease muscle breakdown.
* **Neuroprotective effects:** Some studies suggest that MK-0677 may have neuroprotective effects, potentially protecting the brain against damage from conditions such as stroke and Alzheimer's disease.
* **Pharmacological studies:** MK-0677 is also used in pharmacological research to study the role of the GHS-R and GH in various physiological processes.
**It's important to note:**
* MK-0677 is not currently approved for any medical use.
* While research is promising, there are potential side effects and risks associated with using MK-0677, including water retention, increased risk of blood clots, and possible effects on mood and sleep.
**In summary, MK-0677 is a potent GHS-R agonist with potential applications in treating GHD, metabolic disorders, and enhancing muscle growth, but more research is needed to fully understand its safety and efficacy.**
| ID Source | ID |
|---|---|
| PubMed CID | 646272 |
| CHEMBL ID | 1529889 |
| CHEBI ID | 109622 |
| Synonym |
|---|
| MLS000076103 |
| smr000005918 |
| 1-(3-chloro-4-methoxy-benzenesulfonyl)-piperidine-3-carboxylic acid pyridin-3-ylamide |
| ASN 05984788 |
| MLS002539418 |
| CHEBI:109622 |
| 1-(3-chloro-4-methoxyphenyl)sulfonyl-n-pyridin-3-ylpiperidine-3-carboxamide |
| AKOS000757417 |
| AKOS024316631 |
| HMS2341B15 |
| CHEMBL1529889 |
| Q27188784 |
| 1-(3-chloro-4-methoxyphenyl)sulfonyl-n-(3-pyridinyl)-3-piperidinecarboxamide |
| Class | Description |
|---|---|
| sulfonamide | An amide of a sulfonic acid RS(=O)2NR'2. |
| [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, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 3.5481 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 23.1093 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
| GLS protein | Homo sapiens (human) | Potency | 17.7828 | 0.3548 | 7.9355 | 39.8107 | AID624170 |
| TDP1 protein | Homo sapiens (human) | Potency | 15.4706 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 22.3872 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
| hypothetical protein, conserved | Trypanosoma brucei | Potency | 14.1254 | 0.2239 | 11.2451 | 35.4813 | AID624173 |
| 67.9K protein | Vaccinia virus | Potency | 29.9033 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 39.8107 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 79.4328 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 16.3601 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| huntingtin isoform 2 | Homo sapiens (human) | Potency | 22.3872 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 39.8107 | 0.0398 | 16.7842 | 39.8107 | AID995 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 2.6679 | 0.1683 | 16.4040 | 67.0158 | AID720504 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 2.8184 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 20.4839 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
| geminin | Homo sapiens (human) | Potency | 11.5821 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 15.8489 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 12.5893 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| Glycoprotein hormones alpha chain | Homo sapiens (human) | Potency | 10.0000 | 4.4668 | 8.3448 | 10.0000 | AID624291 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 16.5978 | 1.9953 | 25.5327 | 50.1187 | AID624287; AID624288 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| hormone activity | Glycoprotein hormones alpha chain | Homo sapiens (human) |
| protein binding | Glycoprotein hormones alpha chain | Homo sapiens (human) |
| follicle-stimulating hormone activity | Glycoprotein hormones alpha chain | Homo sapiens (human) |
| G protein activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| adenylate cyclase activator activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| extracellular region | Glycoprotein hormones alpha chain | Homo sapiens (human) |
| extracellular space | Glycoprotein hormones alpha chain | Homo sapiens (human) |
| Golgi lumen | Glycoprotein hormones alpha chain | Homo sapiens (human) |
| follicle-stimulating hormone complex | Glycoprotein hormones alpha chain | Homo sapiens (human) |
| pituitary gonadotropin complex | Glycoprotein hormones alpha chain | Homo sapiens (human) |
| extracellular space | Glycoprotein hormones alpha chain | Homo sapiens (human) |
| plasma membrane | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID651635 | Viability Counterscreen for 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] | ||