LY518674

Names

[ Name ]:
LY518674

[Synonym ]:
2-Methyl-2-[4-[3-[1-(4-Methylbenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl]propyl]phenoxy]propionic acid
Propanoic acid,2-[4-[3-[2,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methyl
2-[4-[3-[4,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid
2-[4-[3-[2,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methyl-propanoic acid

Biological Activity

[Description]:

LY518674 is a potent, selective PPARα antagonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis[1][2][3].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR

Research Areas >> Metabolic Disease

[Target]

EC50: 42 nM (human PPARα)[1]

[In Vivo]

LY518674 reduces triglycerides and increased HDL-C in vivo[2]. LY518674 substantially increases apolipoprotein A-I (apoA-I) turnover without major impact on steady-state levels of apoA-I or high-density lipoprotein-cholesterol (HDL-C) [3].

[References]

[1]. Bravo Y, et al. Identification of the first potent, selective and bioavailable PPARα antagonist. Bioorg Med Chem Lett. 2014 May 15;24(10):2267-72.

[2]. Nissen SE, et al. Effects of a potent and selective PPAR-alpha agonist in patients with atherogenic dyslipidemia or hypercholesterolemia: two randomized controlled trials. JAMA. 2007 Mar 28;297(12):1362-73.

[3]. Khera AV, et al. Potent peroxisome proliferator-activated receptor-α agonist treatment increases cholesterol efflux capacity in humans with the metabolic syndrome. Eur Heart J. 2015 Nov 14;36(43):3020-2.

Chemical & Physical Properties

[ Density]:
1.21g/cm3

[ Boiling Point ]:
575.852ºC at 760 mmHg

[ Molecular Formula ]:
C₂₃H₂₇N₃O₄

[ Molecular Weight ]:
409.47800

[ Flash Point ]:
302.065ºC

[ Exact Mass ]:
409.20000

[ PSA ]:
97.21000

[ LogP ]:
3.34540

[ Index of Refraction ]:
1.594

[ Storage condition ]:
2-8°C

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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