PPAR

Signaling Pathway Map

Research Area

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.

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.

S7484

FH535

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

S4527

Fenofibric acid

Fenofibric acid is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.

S9189New

Oroxin A

Oroxin A, an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.

S9177New

Gypenoside XLIX

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

S8029

WY-14643 (Pirinixic Acid)

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

S1729

Gemfibrozil

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

S5121

Phytol

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.

S4708

Palmitoylethanolamide

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

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.

S5817New

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.

S8025

GSK3787

GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.

S2505

Rosiglitazone maleate

Rosiglitazone, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ with IC50 of 42 nM.

S2556

Rosiglitazone

Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action.

S2590

Pioglitazone

Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.

S5812New

Choline Fenofibrate

Choline fenofibrate is a newly developed choline salt of fenofibric acid, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist.

S8770New

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.

S9199New

Pseudoginsenoside F11

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

S8020

GW0742

GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.

S2665

Ciprofibrate

Ciprofibrate is a peroxisome proliferator-activated receptor agonist.

S4159

Bezafibrate

Bezafibrate is the first clinically tested dual and pan-PPAR co-agonism.

S4207

Clofibric Acid

Clofibric acid is a PPARα agonist and hypolipidemic agent.

S1794

Fenofibrate

Fenofibrate (Tricor, Trilipix) is a compound of the fibrate class and fibric acid derivative.

S2075

Rosiglitazone HCl

Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

S3786

Glabridin

Glabridin, 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.

S8432

Troglitazone (CS-045)

Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth.

S3878

Bavachinin

Bavachinin 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).

S3720

Elafibranor

Elafibranor 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.

S5615

Cardarine (GW501516)

GW501516 is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.

S3868

Harmine

Harmine is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.

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.

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.

S7484

FH535

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

S4527

Fenofibric acid

Fenofibric acid is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.

Catalog No. Information Product Use Citations Product Validations
S9189New

Oroxin A

Oroxin A, an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.

S9177New

Gypenoside XLIX

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

S8029

WY-14643 (Pirinixic Acid)

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

S1729

Gemfibrozil

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

S5121

Phytol

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.

S4708

Palmitoylethanolamide

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

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.

S5817New

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.

S8025

GSK3787

GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.

Catalog No. Information Product Use Citations Product Validations
S2505

Rosiglitazone maleate

Rosiglitazone, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ with IC50 of 42 nM.

S2556

Rosiglitazone

Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action.

S2590

Pioglitazone

Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.

S5812New

Choline Fenofibrate

Choline fenofibrate is a newly developed choline salt of fenofibric acid, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist.

S8770New

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.

S9199New

Pseudoginsenoside F11

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

S8020

GW0742

GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.

S2665

Ciprofibrate

Ciprofibrate is a peroxisome proliferator-activated receptor agonist.

S4159

Bezafibrate

Bezafibrate is the first clinically tested dual and pan-PPAR co-agonism.

S4207

Clofibric Acid

Clofibric acid is a PPARα agonist and hypolipidemic agent.

S1794

Fenofibrate

Fenofibrate (Tricor, Trilipix) is a compound of the fibrate class and fibric acid derivative.

S2075

Rosiglitazone HCl

Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

S3786

Glabridin

Glabridin, 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.

S8432

Troglitazone (CS-045)

Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth.

S3878

Bavachinin

Bavachinin 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).

S3720

Elafibranor

Elafibranor 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.

S5615

Cardarine (GW501516)

GW501516 is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.

Catalog No. Information Product Use Citations Product Validations
S3868

Harmine

Harmine is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.