PPARα Selective Inhibitors | Activators | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S4527 Fenofibric acid

Fenofibric acid (NSC 281318, Trilipix, FNF acid) is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.

Selective
S5121 Phytol

Phytol (Trans-Phytol), a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.

Selective
S9674 Saroglitazar

Saroglitazar (Lipaglyn, ZYH1) is an agonist of peroxisome proliferator-activated receptor (PPAR) with EC50 of 0.65 pM and 3 nM for hPPARα and hPPARγ in HepG2 cells, respectively.

Selective hPPARα, EC50: 0.65 pM
S0170 BMS-687453

BMS-687453 (compound 2) is a potent and selective agonist of PPARα with EC50 of 10 nM and IC50 of 260 nM for human PPARα.

Selective PPARα, IC50: 260 nM; PPARα, EC50: 10 nM
S2798 GW6471

GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.

Selective PPARα, IC50: 0.24 μM
S8029 WY-14643 (Pirinixic Acid)

WY 14643 (Pirinixic Acid, NSC 310038) is a potent peroxisome proliferator and activator of PPARα with EC50 of 1.5 μM.

Selective PPARα, EC50: 1.5 μM
S4708 Palmitoylethanolamide

Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.

Selective PPARα, EC50: 3.1 μM
S1729 Gemfibrozil

Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.

Selective
S1794 Fenofibrate (NSC-281319)

Fenofibrate (NSC-281319) is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.

Selective
S4207 Clofibric Acid

Clofibric acid is a PPARα agonist and hypolipidemic agent.

Selective
S3720 Elafibranor

Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.

Pan
S2915 GW9662

GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.

Pan PPARα, IC50: 32 nM
S9723 CDDO-Im

CDDO-Im (CDDO-Imidazolide, RTA-403, TP-235) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo.

Pan PPARα, Ki: 232 nM
S8770 Lanifibranor (IVA-337)

Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively.

Pan PPARα, EC50: 1537 nM
S3878 Bavachinin

Bavachinin (7-O-Methylbavachin) is a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).

Pan PPARα, Ki: 7.881 μM