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GW7647 | GW7647 : Agonist of PPARA
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PPARA
  • EC50:6 nM
  • EC50:51.8 nM
  • INH:inhibition of proliferation
  • Activity:600 nM
Agonist
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity >100-fold over PPARγ and PPARδ EC50 1100 nM PPARγ EC50 6200 nM PPARδ

Potency
Cellular
In Vitro

PPARA

Mode of Action: Agonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/S0960-894X(01)00188-3

In Vivo Validations

Rat
Dose: 3 mg/Kg BID
Route of delivery: Oral
Target engagement assay: Oral administration to cholesterol/cholic acid-fed rats5 for 4 days resulted in a 60% increase in HDL-cholesterol, a 60% decrease in triglycerides, and a 40% decrease in serum apolipoprotein CIII.

DOI Reference: 10.1016/S0960-894X(01)00188-3

Hamster
Dose: 3 mg/Kg BID
Route of delivery: Oral
Target engagement assay: Oral administration to cholesterol/cholic acid-fed hamsters for 7 days resulted in a 93% decrease in triglycerides.

DOI Reference: 10.1016/S0960-894X(01)00188-3

Chemical Information

Molecular Formula C29H46N2O3S
SMILEs CC(C)(Sc1ccc(CCN(CCCCC2CCCCC2)C(=O)NC2CCCCC2)cc1)C(=O)O
InChI 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)
Molecular weight 502.32 Da
AlogP 0.0
HBond acceptors 5
HBond donors 2
Atoms 81

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 22 Nov 2022 )
Cellular Use Rating
In Model Organisms
This is perhaps the most selective agonist for PPARa and is potent and efficacious both in vitro and in vivo. The compound is orally bioavailable in rat with dose promotional exposure at 1 and 10 mg/kg...
by SERP
(on 1 Dec 2022 )
Cellular Use Rating
In Model Organisms
This probe shows high selectivity for PPARa using cell-based reporter assays for PPARs alpha/beta/gamma, and in vivo studies using multiple species (rat, hamster) have demonstrated expected alterations...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria