Inhibitor/Activator
| Cat.No. | Name | Information |
|---|---|---|
| M5940 | Rosiglitazone HCl | Rosiglitazone HCl is a hypoglycemic compound that stimulates insulin secretion by binding to PPAR receptors in fat cells. |
| M2748 | GW9662 | GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM, with at least 100 to 1000-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ. |
| M1880 | WY 14643 (Pirinixic Acid) | WY 14643 (Pirinixic Acid) is a potent and selective, peroxisome proliferator-activated receptor-α (PPARα) agonist. |
| M2335 | ZLN005 | ZLN005 is a novel and potent small molecule PGC-1α transcriptional activator. |
| M5878 | Pioglitazone HCl | Pioglitazone HCl is a selective peroxisome proliferator-activated receptor-gamma (PPARgamma) agonist, used to treat diabetes. |
| M3283 | Pioglitazone | Pioglitazone (U 72107) is a selective peroxisome proliferator-activated receptor gamma stimulator. |
| M1894 | Rosiglitazone | Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50=60 nM, Kd=40 nM). Rosiglitazone is an TRPC5 activator (EC50=30 μM) and TRPM3 inhibitor. |
| M2747 | GW7647 | GW7647 is a potent and highly selective PPARα agonist with EC50 of 6 nM. |
| M6723 | Fenofibrate | Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate inhibited cytochrome P450 subtype, with IC50 of 0.2, 0.7, 9.7, 4.8, and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively. |
| M9747 | Lanifibranor | Lanifibranor (IVA-337) is a peroxisome proliferator-activated receptors (PPAR) agonist, with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively. |
| M40989 | Azemiglitazone potassium | Azemiglitazone potassium is a thiazolidinediones that binds to PPARγ with an IC50 value of 18.25 μM. It also modulates the mitochondrial pyruvate carrier (MPC). It can be used in studies related to non-alcoholic steatohepatitis (NASH). |
| M40982 | PXL065 | PXL065 is a PPARγ agonist that can be used in studies related to non-alcoholic steatohepatitis (NASH). |
| M38943 | Caulophyllogenin | Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC50 of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation. |
| M30723 | LT175 | LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC50=0.22 μm; mPPARα:EC50=0.26 μm; hPPARγ:EC50=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties. |
| M30564 | Chiglitazar | Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively. |
| M30143 | Naveglitazar | Naveglitazar (LY519818) is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models. |
| M29926 | Muraglitazar | Muraglitazar is a PPAR α/γ dual agonist for the research of type 2 diabetes and associated dyslipidemia. Muraglitazar shows potent activity in vitro at human PPARα (EC50 = 320 nM) and PPARγ(EC50 = 110 nM). |
| M29897 | AMG131 | AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM). |
| M29616 | Arhalofenate | Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes. |
| M29446 | LJ570 | LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively. |
| M29393 | Inolitazone | Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition. |
| M29287 | Edaglitazone | Edaglitazone is a potent, selective and orally active PPARγ agonist, with EC50s of 35.6 nM and 1053 nM for PPARα and PPARγ, respectively. Edaglitazone displays antiplatelet, antidiabetic and anti-hyperglycemic activity. |
| M29282 | KRP-297 | KRP-297 is a PPARα and PPARγ agonist potentially for the research of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver. |
| M29209 | Bocidelpar | Bocidelpar is a modulator of peroxisome proliferator-activated receptor delta (PPAR-δ). Bocidelpar improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy (DMD) muscle cells. |
| M29186 | SR 16832 | SR 16832 is a dual site covalent PPARγ inhibitor that acts at orthosteric and allosteric sites. |
| M29067 | Farglitazar | Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients. |
| M29032 | FK614 | FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes. |
| M28361 | Darglitazone | Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research. |
| M28316 | MHY908 | MHY908 is a potent dual agonist of PPARα and PPARγ. MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity. |
| M28026 | DS-6930 | DS-6930 is a potent and selective agonist of PPARγ, with an EC50 of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes. |
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