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PPAR Agonists/Antagonist

Other Metabolism Related Inhibitors

Dehydrogenase Transferase DPP Aminopeptidase Procollagen C Proteinase P450 (e.g. CYP17) Phospholipase (e.g. PLA) Factor Xa PDE DHFR

Isoform-selective Products

PPARα PPARβ/δ PPARγ PPARδ

Cat.No.	Product Name	Information	Product Use Citations	Product Validations
S2871	T0070907	T0070907 is a potent inhibitor of PPARγ (peroxisome proliferator activator receptor γ ) that induces G2/M arrest and enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. It also acts as an antagonist of PPARγ that suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms.	Nucleic Acids Res, 2025, 53(14)gkaf669 Cell Rep Med, 2025, 6(10):102373 Apoptosis, 2025, 30(5-6):1391-1409
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.	J Extracell Vesicles, 2025, 14(8):e70143 Stem Cell Res Ther, 2025, 16(1):347 Genes Dis, 2025, 12(3):101333
S2556	Rosiglitazone (BRL 49653)	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. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.	Signal Transduct Target Ther, 2025, 10(1):394 Nat Commun, 2025, 16(1):6241 Lab Invest, 2025, 105(4):104103
S2590	Pioglitazone (U-72107)	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.	Front Pharmacol, 2025, 16:1559446 Signal Transduct Target Ther, 2024, 9(1):257 Cell Commun Signal, 2024, 22(1):266
S2798	GW6471	GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.	Mol Cancer, 2025, 24(1):34 Cell Mol Immunol, 2025, 10.1038/s41423-025-01338-y Apoptosis, 2025, 30(5-6):1391-1409
S2505	Rosiglitazone maleate	Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. This compound also modulates TRP channels and induces autophagy. It prevents ferroptosis.	Stem Cell Reports, 2022, 17(11):2531-2547 Cell Death Dis, 2021, 12(11):972 Antioxidants (Basel), 2021, 10(2)155
S2075	Rosiglitazone HCl	Rosiglitazone HCl is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.	J Immunother Cancer, 2024, 12(11)e009805 Stem Cell Reports, 2022, 17(11):2531-2547 Cell Death Dis, 2021, 12(11):972
S8029	WY-14643 (Pirinixic Acid)	WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM.	Mol Med, 2025, 31(1):153 Int J Mol Sci, 2025, 26(3)1051 Front Pharmacol, 2024, 15:1366479
S1794	Fenofibrate	Fenofibrate is a compound of the fibrate class and fibric acid derivative. This compound is a selective agonist of PPARα with EC50 of 30 μM. It 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. This chemical induces autophagy.	J Cell Mol Med, 2025, 29(7):e70524 J Immunother Cancer, 2024, 12(11)e009805 Heliyon, 2024, 10(11):e31861
S8025	GSK3787	GSK3787 is a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.	JACC Basic Transl Sci, 2025, 10(7):101222 Drug Des Devel Ther, 2024, 18:4799-4824 Cell Discov, 2023, 9(1):54
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Signaling Pathway Map