ppar-γ

Darglitazone (CP-86325) is a potent, selective agonist of PPAR-γ with antidiabetic actions. Darglitazone is effective in controlling blood glucose and lipid metabolism.

Candesartan (CV 11974) is an angiotensin II receptor blocker widely used in the treatment of hypertension and heart failure.

Arhalofenate (JNJ 39659100) is a selective partial agonist of peroxisome proliferator-activated receptor PPARγ. It is used for the treatment of type 2 diabetes.

β-Carotene (Provitamin A) is a naturally-occurring retinol (vitamin A) precursor obtained from certain fruits and vegetables with potential antineoplastic and chemopreventive activities. As an anti-oxidant, beta carotene inhibits free-radical damage to DNA.

Pioglitazone (U 72107) is a PPARγ agonist with EC50 of 0.93 and 0.99 μM on human and mouse PPARγ, respectively, and has selective and oral activity. Pioglitazone can be used in diabetes research.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

5-Aminosalicylic Acid (5-ASA) is a specific PPARγ agonist and also inhibits P21-activated kinase 1(PAK1) and NF-Κb. 5-Aminosalicylic Acid has anti-cancer and anti-inflammatory activities. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

Retinoic acid (Tretinoin), a metabolite of vitamin A, is a natural agonist of the retinoic acid receptor RAR and inhibits RARα/β/γ (IC50=14 nM). Retinoic acid induces cellular differentiation, reduces cellular proliferation, and inhibits tumorigenesis.

GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect.

Troglitazone (Romglizone) is a PPARγ agonist with anti-inflammatory and anti-tumor activity.

T0070907(IC50=1 nM) , an effective and specific PPARγ inhibitor, with the >800-fold selectivity over PPARα and PPARδ.

GW6471 is an antagonist of PPARα with IC50 of 0.24 μ M. GW6471 enhances the binding affinity of the PPAR α ligand-binding domain to the co-repressor proteins SMRT and NCoR.

Sakuranetin, a flavanone phytoalexin from ultraviolet-irradiated rice leaves, it has antifungal, antimutagenic, anti-inflammatory and antioxidant effects

RG-12525(NID 525) is an orally available, selective and competitive leukotriene D (LTD) antagonist that inhibits LTC4, LTD4 and LTE4-induced contraction of guinea pig thin-walled bands, with IC50 values of 2.6 nM, 2.5 nM, and 7 nM, respectively.RG-12525 inhibits CYP3A4, with a Ki value of 0.5 µM. RG-12525 is a novel and potent PPAR-γ agonist (IC50 value of about 60 nM) with species specificity for the study of asthma.

Tesaglitazar is a potent and selective peroxide PPARα / γ receptor dual agonist with a more potent affinity for PPARγ than PPARα, The EC50 values for rat PPARα and human PPARα were 13.4 μM and 3.6 μM, respectively, and 0.2 μM for rat PPARγ and human PPARγ. Tesaglitazar induced DNA synthesis and fibrosarcoma formation in rat subcutaneous mesenchymal cells.

Muraglitazar (BMS-298585) is a dual agonist of PPARα/γ that exerts metabolic regulatory effects including lipid modulation, glucose reduction, improvement of insulin resistance, and weight loss. It is indicated for the treatment of type 2 diabetes and associated dyslipidemia. Muraglitazar exhibits potent in vitro activity against human PPARα (EC50 = 320 nM) and PPARγ (EC50 = 110 nM).

Farglitazar (GI-262570) is a PPAR-γ agonist and insulin sensitizer that inhibits stellate cell activation by activating receptor γ via oxidative enzymes proliferators and is used in the study of diabetes.

CGS 15435 is a potent thromboxen (TxA2) synthetase inhibitor (IC50: 1 nM). CGS 15435 acts on PGI2 synthase, cyclooxygenase and liposynthase with much less selectivity than on thromboxin synthase.

Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 μM. Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively).

Furegrelate sodium (U-63557A) is a selective thromboxane synthase inhibitor with oral activity. Furegrelate sodium(U-63557A) inhibits thromboxane A2 (TXA2) synthase in human platelet microsomes with an IC50 of 15 nM.

FUREGRELATE, a thromboxane A2 (TxA2) synthase inhibitor, blunts the development of pulmonary arterial hypertension in neonatal piglets.

KD-3010 (Kalypsys) is an orally active potent and selective PPARδ agonist for the study of liver injury.

LCB-2853 is a potent thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor antagonist with antiplatelet aggregation, antivasospasm, and antithrombotic effects.

Peliglitazar racemate(BMS 426707-01 racemate) is the racemate of Peliglitazar.Peliglitazar racemate may be used as a potential antidiabetic and anti-obesity agent.