Details
Stereochemistry | ACHIRAL |
Molecular Formula | C29H46N2O3S |
Molecular Weight | 502.752 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(SC1=CC=C(CCN(CCCCC2CCCCC2)C(=O)NC3CCCCC3)C=C1)C(O)=O
InChI
InChIKey=PKNYXWMTHFMHKD-UHFFFAOYSA-N
InChI=1S/C29H46N2O3S/c1-29(2,27(32)33)35-26-18-16-24(17-19-26)20-22-31(28(34)30-25-14-7-4-8-15-25)21-10-9-13-23-11-5-3-6-12-23/h16-19,23,25H,3-15,20-22H2,1-2H3,(H,30,34)(H,32,33)
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/11354382 | https://www.ncbi.nlm.nih.gov/pubmed/16038868Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/14557369
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11354382 | https://www.ncbi.nlm.nih.gov/pubmed/16038868
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/14557369
GW7647 is a potent and highly selective PPARα agonist (EC50 values are 6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors respectively). GW7647 has being shown to protect the heart from ischemia/reperfusion injury in mouse model. GW7647 attenuated ischemia/reperfusion-induced release of multiple proinflammatory cytokines and inhibited neutrophil accumulation and myocardial expression of matrix metalloproteinases-9 and -2. Furthermore, GW7647 inhibited nuclear factor-kappaB activation in the heart, accompanied by enhanced levels of inhibitor-kappaBalpha.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16997973 | https://www.ncbi.nlm.nih.gov/pubmed/19386271
Curator's Comment: GW 7647 reduced nocifensive behaviors elicited in mice by intraplantar (i.pl.) injection of formalin or i.p. injection of magnesium sulfate.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL239 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11354382 |
6.0 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/14557369
Mice: GW7647, was administered by mouth for 2 days, and the third dose was given 1 hour before ischemia. GW7647 at 1 and 3 mg x kg(-1) x d(-1) reduced infarct size by 28% and 35%, respectively
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11916905
In mature human myotubes, 48-h treatment with 10-1,000 nmol/l GW7647 increased oleate oxidation dose-dependently, up to threefold.
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SUBSTANCE RECORD