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GW 9578

Names

[ CAS No. ]:
247923-29-1

[ Name ]:
GW 9578

[Synonym ]:
2-{[4-(2-{[(2,4-Difluorophenyl)carbamoyl](heptyl)amino}ethyl)phenyl]sulfanyl}-2-methylpropanoic acid
gsk9578
unii-h32abl87x4
Propanoic acid, 2-[[4-[2-[[[(2,4-difluorophenyl)amino]carbonyl]heptylamino]ethyl]phenyl]thio]-2-methyl-
gw 9578

Biological Activity

[Description]:

GW9578 is a subtype-selective PPARα agonist (EC50s of 5 and 50 nM for murine and human PPAR-α) with potent lipid-lowering activity[1][2].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR
Research Areas >> Inflammation/Immunology
Research Areas >> Metabolic Disease

[Target]

mouse PPARα:5 nM (EC50)

h-PPARα:50 nM (EC50)


[In Vitro]

GW9578 exhibits activities on Murine PPAR-α, PPAR-γ, and PPAR-δ with EC50s of 0.005, 1.5, 2.6 μm, respectively. GW9578 exhibits activities on Human PPAR-α, PPAR-γ, and PPAR-δ with EC50s of 0.05, 1, and 1.4 μm, respectively[2]. Treatment of the CD8+ T-cell line, TK.1 cells with GW9578 (10 nM-1 μM; for 24 hours) is able to induce a dose-dependent increase in the amount of relative luciferase activity[3]. Treatment of murine T-cell thymoma EL-4 T cells with GW9578 (10 nM-10 μM; for 2 hours) leads to a significant decrease in IL-2 production compared with control cells[3].

[References]

[1]. P J Brown, et al. A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity. J Med Chem. 1999 Sep 23;42(19):3785-8.

[2]. Alexandre Trifilieff, et al. PPAR-alpha and -gamma but not -delta agonists inhibit airway inflammation in a murine model of asthma: in vitro evidence for an NF-kappaB-independent effect. Br J Pharmacol. 2003 May;139(1):163-71.

[3]. Dallas C Jones, et al. Nuclear receptor peroxisome proliferator-activated receptor alpha (PPARalpha) is expressed in resting murine lymphocytes. The PPARalpha in T and B lymphocytes is both transactivation and transrepression competent. J Biol Chem. 2002 Mar 1;277(9):6838-45.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
641.7±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H34F2N2O3S

[ Molecular Weight ]:
492.622

[ Flash Point ]:
341.9±31.5 °C

[ Exact Mass ]:
492.225830

[ PSA ]:
94.94000

[ LogP ]:
6.87

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.574

Related Compounds