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Details

Stereochemistry ACHIRAL
Molecular Formula C23H21F3N2O4S
Molecular Weight 478.484
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GW-590735

SMILES

CC1=C(SC(=N1)C2=CC=C(C=C2)C(F)(F)F)C(=O)NCC3=CC=C(OC(C)(C)C(O)=O)C=C3

InChI

InChIKey=ILUPZUOBHCUBKB-UHFFFAOYSA-N
InChI=1S/C23H21F3N2O4S/c1-13-18(33-20(28-13)15-6-8-16(9-7-15)23(24,25)26)19(29)27-12-14-4-10-17(11-5-14)32-22(2,3)21(30)31/h4-11H,12H2,1-3H3,(H,27,29)(H,30,31)

HIDE SMILES / InChI

Molecular Formula C23H21F3N2O4S
Molecular Weight 478.484
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

GW 590735 is a selective and potent agonist of peroxisome proliferator-activated receptor alpha (PPARα), a ligand-activated transcription factor that plays a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein. GW 590735 was in phase II clinical trial for the treatment of dyslipidemia, but that study was discontinued.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
4.0 nM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
1461 ng/mL
3 mg/kg single, oral
GW-590735 plasma
Rattus norvegicus

T1/2

ValueDoseCo-administeredAnalytePopulation
2.4 h
2.7 mg/kg single, intravenous
GW-590735 plasma
Rattus norvegicus

PubMed

Sample Use Guides

In Vivo Use Guide
eight weeks treatment with 1µg to 20µg daily doses of GW590735 in otherwise healthy subjects with low HDLc, mildly to moderately elevated TG, and normal LDLc
Route of Administration: Unknown
In Vitro Use Guide
Unknown
Substance Class Chemical
Record UNII
QKY617BBX5
Record Status Validated (UNII)
Record Version