naveglitazar: LY-519818 is the (alpha-S)-isomer; an antidiabetic agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9888484 |
| CHEMBL ID | 181954 |
| CHEBI ID | 188591 |
| SCHEMBL ID | 2827844 |
| MeSH ID | M0507549 |
| Synonym |
|---|
| ly-818 |
| naveglitazar |
| ly-9818 |
| ly-519818 |
| bdbm50157056 |
| (s)-2-methoxy-3-{4-[3-(4-phenoxy-phenoxy)-propoxy]-phenyl}-propionic acid |
| naveglitazar (usan/inn) |
| 476436-68-7 |
| D08949 |
| ly9818 |
| ly519818 |
| CHEMBL181954 , |
| CHEBI:188591 |
| (2s)-2-methoxy-3-[4-[3-(4-phenoxyphenoxy)propoxy]phenyl]propanoic acid |
| unii-y995m7gm0g |
| benzenepropanoic acid, alpha-methoxy-4-(3-(4-phenoxyphenoxy)propoxy)-, (alphas)- |
| alpha-methoxy-4-(3-(4-phenoxyphenoxy)propoxy)benzenepropionic acid |
| (2s)-2-methoxy-3-(4-(3-(4-phenoxyphenoxy)propoxy)phenyl)propanoic acid |
| naveglitazar [usan:inn] |
| ccris 9448 |
| ly 9818 |
| ly 519818 |
| y995m7gm0g , |
| naveglitazar [inn] |
| naveglitazar [usan] |
| benzenepropanoic acid, .alpha.-methoxy-4-(3-(4-phenoxyphenoxy)propoxy), (.alpha.s) |
| SCHEMBL2827844 |
| DB12662 |
| (s)-2-methoxy-3-(4-(3-(4-phenoxyphenoxy)propoxy)phenyl)propanoic acid |
| CS-0021934 |
| HY-U00036A |
| Q27294403 |
| DTXSID70870358 |
| AKOS040753217 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Using the recently published preclinical data of naveglitazar, an allometric method was used to predict the human pharmacokinetic parameters (CL/F and Vss/F)." | ( Allometric prediction of the human pharmacokinetic parameters for naveglitazar. Ahlawat, P; Srinivas, NR, ) | 0.13 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " After oral administration of [(14)C]naveglitazar, naveglitazar was well absorbed and moderately metabolized in all species evaluated, with total recoveries of radioactivity ranging from 90 to 96%." | ( The disposition and metabolism of naveglitazar, a peroxisome proliferator-activated receptor alpha-gamma dual, gamma-dominant agonist in mice, rats, and monkeys. Annes, WF; Gillespie, TA; Hadden, CE; Jackson, DA; Johnson, JT; Peterson, BC; Yi, P, 2007) | 0.34 |
| Class | Description |
|---|---|
| aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
| [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 | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glutamate receptor ionotropic, kainate 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.9160 | 0.0070 | 0.9821 | 7.0000 | AID242341 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | IC50 (µMol) | 0.0340 | 0.0050 | 1.2051 | 10.0000 | AID242406; AID665205 |
| Glutamate receptor ionotropic, kainate 2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.9160 | 0.0070 | 1.0132 | 7.0000 | AID242341 |
| Glutamate receptor ionotropic, kainate 3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.9160 | 0.0070 | 1.0132 | 7.0000 | AID242341 |
| Glutamate receptor ionotropic, kainate 4 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.9160 | 0.0070 | 1.0132 | 7.0000 | AID242341 |
| Peroxisome proliferator-activated receptor delta | Homo sapiens (human) | IC50 (µMol) | 1.9151 | 0.0010 | 0.8505 | 6.3100 | AID242341; AID665204 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | IC50 (µMol) | 2.7106 | 0.0005 | 0.8269 | 6.3100 | AID242373; AID665203 |
| Glutamate receptor ionotropic, kainate 5 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.9160 | 0.0070 | 1.0132 | 7.0000 | AID242341 |
| [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) |
|---|---|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | EC50 (µMol) | 0.3805 | 0.0000 | 0.9922 | 10.0000 | AID240232; AID717061 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | EC50 (µMol) | 2.8080 | 0.0006 | 1.6074 | 10.0000 | AID240227; AID717062 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID239803 | Mean percent of maximum efficacy against human peroxisome proliferator-activated receptor gamma | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | 2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents. |
| AID239802 | Mean percent of maximum efficacy against human peroxisome proliferator-activated receptor alpha | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | 2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents. |
| AID242406 | Mean inhibitory concentration against human peroxisome proliferator-activated receptor gamma | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | 2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents. |
| AID240227 | Mean effective concentration against human peroxisome proliferator activated receptor alpha | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | 2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents. |
| AID665205 | Agonist activity at PPARgamma | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Activity landscape modeling of PPAR ligands with dual-activity difference maps. |
| AID246887 | In vivo effective dose value in NIDDM animal model (ZDF rat) | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | 2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents. |
| AID665203 | Agonist activity at PPARalpha | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Activity landscape modeling of PPAR ligands with dual-activity difference maps. |
| AID242341 | Mean inhibitory concentration against human peroxisome proliferator-activated receptor delta | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | 2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents. |
| AID240232 | Mean effective concentration against human peroxisome proliferator-activated receptor gamma | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | 2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents. |
| AID717062 | Agonist activity at GAL4-fused PPARalpha assessed as transcriptional activity by cell based assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1). |
| AID665204 | Agonist activity at PPARdelta | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Activity landscape modeling of PPAR ligands with dual-activity difference maps. |
| AID242373 | Mean inhibitory concentration against human peroxisome proliferator activated receptor alpha | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | 2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents. |
| AID717061 | Agonist activity at GAL4-fused PPARgamma assessed as transcriptional activity by cell based assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1). |
| [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 | 4 (66.67) | 29.6817 |
| 2010's | 2 (33.33) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| 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 | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||