PPAR

Inhibitory Selectivity

Isoform-specific Inhibitors

PPAR Products

New PPAR Products
Catalog No. Information Product Use Citations Product Validations
S2871

T0070907

T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells.

S7767

AZ6102

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.

S2798

GW6471

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

S7484

FH535

FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.

S5824

Cinnamyl alcohol

Cinnamyl alcohol is a naturally occurring compound that is found within cinnamon. Cinnamyl alcohol can be significantly attenuated the enhanced expression of obesity-related proteins PPARγ in MDI medium-cultivated 3T3-L1 cells.

S9129

20(S)-Ginsenoside Rh1

20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.

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.

S3290New

Procyanidin B2

Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model.

S9723New

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.

S3875

Alpinetin

Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities. Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.

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.

S9177

Gypenoside XLIX

Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.

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.

S5817

GSK0660

GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.

S9199

Pseudoginsenoside F11

Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.

S3786

Glabridin

Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.

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.

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.

S9480

Raspberry Ketone

Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity.

S6906

Capric acid

Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.

Catalog No. Information Product Use Citations Product Validations
S2871

T0070907

T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells.

S7767

AZ6102

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.

S2798

GW6471

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

S7484

FH535

FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.

S5824

Cinnamyl alcohol

Cinnamyl alcohol is a naturally occurring compound that is found within cinnamon. Cinnamyl alcohol can be significantly attenuated the enhanced expression of obesity-related proteins PPARγ in MDI medium-cultivated 3T3-L1 cells.

S9129

20(S)-Ginsenoside Rh1

20(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.

Catalog No. Information Product Use Citations Product Validations
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.

S3290New

Procyanidin B2

Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model.

S9723New

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.

S3875

Alpinetin

Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities. Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.

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.

S9177

Gypenoside XLIX

Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.

Catalog No. Information Product Use Citations Product Validations
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.

S5817

GSK0660

GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.

Catalog No. Information Product Use Citations Product Validations
S9199

Pseudoginsenoside F11

Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.

S3786

Glabridin

Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.

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.

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.

S9480

Raspberry Ketone

Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity.

Catalog No. Information Product Use Citations Product Validations
S6906

Capric acid

Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.