Catalog No.
Product Name
Application
Product Information
Citations
- 6-?Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent, downregulates mRNA levels of PPAR γ and C/EBPα, as well as PPAR γ target protein such as LPL, CD36, aP2, and LXRα.
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PPAR-δ agonist
Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases. -
peptidoleukotrienes antagonist
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 ?M. -
PPAR-α agonist
Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis. -
PPARα/ PPARγ1 agonist
Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM. -
PPARδ agonist
PPARδ agonist is a PPARδ agonist extracted from patent US20180071304, compound example 10. - 4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.
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PPAR gamma agonist
Leriglitazone is a peroxisome proliferator activated receptor (PPAR) gamma agonist. -
MPC inhibitor
MSDC-0602, a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and are effective for treatment of type 2 diabetes with reducing risk of PPARγ-mediated side effects. -
PPARγ modulator
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus. -
PPAR-γ partial agonist
Balaglitazone is a novel partial agonist of PPAR-gamma (γ). -
CYP2C19/CYP2B6 inhibitor
Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia. -
PPARγ agonist
Inolitazone dihydrochloride is a novel high-affinity PPARγ agonist, which activates PPARγ with an EC50 about 1/50 that of rosiglitazone and has no effect on RIE cells. -
anti-cancer agent
Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules. Falnidamol is a pyrimido-pyrimidine compound with anti-cancer activity. -
PPAR-γ antagonist
T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2. -
PPARγ agonist
Pioglitazone selectively stimulates the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-γ) and to a lesser extent PPAR-α. -
PPAR agonist
Bezafibrate is the first clinically tested dual and pan-PPAR co-agonist. -
PPARβ/δ inverse agonist
DG-172 is an orally active potent PPARβ/δ inverse agonist (IC50 = 26.9 nM). DG-172 inhibits Angptl4 gene expression in mouse myoblasts (IC50 = 9.5 nM) in vitro. -
PPARγ agonist
Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. -
PPAR agonist
BMS-687453 is a potent and selective peroxisome proliferator activated receptor (PPAR) alpha agonist, with an EC(50) of 10 nM for human PPARalpha and approximately 410-fold selectivity vs human PPARgamma in PPAR-GAL4 transactivation assays. - Fenofibric acid is a fibrate that acts as a lipid-lowering agent, decreasing low-density lipoprotein cholesterol and triglycerides.
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PPARγ Inhibitor
Soyasaponin Ab is a potent PPARγ inhibitor with oral bioavailability. It effectively suppresses PPARγ transcriptional activity and induces apoptosis at elevated concentrations. This compound exhibits a range of biological activities, including anti-obesity, anti-oxidation, anti-inflammation, and anti-aging effects. Additionally, Soyasaponin Ab has been shown to mitigate memory impairment induced by Scopolamine, making it a valuable reagent for research in metabolic and neuroprotective applications. -
PPARγ Inhibtior
Perfluorotetradecanoic acid (PFTeDA) is a potent PPARγ inhibitor, demonstrating a binding affinity to the human PPARγ ligand-binding domain with an IC50 of 22.8 μM and a Kd of 157.8 μM. It has been shown to impair Leydig cell function through the induction of oxidative stress and apoptosis. Additionally, PFTeDA stimulates corticosterone biosynthesis while inhibiting aldosterone production, making it a valuable tool for researching steroidogenesis and related metabolic pathways. -
PPARγ Ligand
CAY10506 is a potent ligand of peroxisome proliferator-activated receptor gamma (PPARγ) that induces cell death and reactive oxygen species (ROS) production through a PPARγ-dependent mechanism. This compound demonstrates radiosensitizing properties, enhancing apoptosis induced by gamma radiation and facilitating caspase-3-mediated cleavage of poly (ADP-ribose) polymerase (PARP). CAY10506 is applicable in cancer research, particularly in studies focused on PPARγ signaling pathways and radiation therapy augmentation. -
PPARγ Agonist
GW7845 is a non-thiazolidinedione, tyrosine-derived agonist of PPARγ that exhibits oral bioactivity. It effectively inhibits voltage-dependent calcium channels (VDCC), relaxing pressurized arteries with an IC50 of 3 μM when using Ba2+ as the charge carrier. Additionally, GW7845 induces apoptosis in a manner that is dependent on mitochondria and the apoptosome, leading to rapid mitochondrial membrane depolarization and the release of cytochrome c in primary pro-B cells and BU-11 cells. This compound is useful for research into metabolic disorders and cardiovascular health. -
PPARγ Modulator
GED 0507-34-Levo is an orally active modulator of PPARγ. This compound effectively downregulates the expression of TGF-β, Smad3, IL-13, and CTGF in colon tissue. GED 0507-34-Levo has demonstrated therapeutic potential in improving symptoms of DSS-induced chronic colitis and associated fibrosis, making it a valuable tool for research in inflammatory bowel diseases and fibrotic disorders. -
PPAR Activator
Rosiglitazone sodium is a potent and selective activator of the peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting EC50 values of 30 nM, 100 nM, and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, with a Kd of approximately 40 nM. In addition to its role as a PPARγ activator, Rosiglitazone sodium functions as a modulator of transient receptor potential (TRP) channels, specifically inhibiting TRP melastatin 2 (TRPM2) and TRPM3, while activating TRP canonical 5 (TRPC5). This compound is utilized in research related to metabolic disorders, obesity, and other conditions linked to PPARγ signaling. -
Pan-PPAR Agonist, HIF-1α Inhibitor
Bavachinin is a pan-peroxisome proliferator-activated receptor (PPAR) agonist and a HIF-1α inhibitor, demonstrating IC50 values of 21.043 μM, 12.819 μM, and 0.622 μM for PPAR-α, PPAR-β/δ, and PPAR-γ, respectively. This compound exhibits significant antitumor activity against non-small cell lung cancer through its modulation of PPAR-γ. Additionally, Bavachinin possesses notable anti-inflammatory and anti-angiogenic properties, making it a valuable tool for research in cancer and metabolic disorders. Its oral bioavailability further supports its utility in various biological studies. -
PPARG Inverse Agonist
FX-909 is a covalent inverse agonist of peroxisome proliferator-activated receptor gamma (PPARG), functioning through modulation of receptor activity. This compound exhibits promising biological activity by inhibiting PPARG-mediated signaling pathways, which are often implicated in cancer progression. FX-909 is utilized in cancer research to investigate the effects of PPARG inhibition on tumor growth and survival, providing insights into potential therapeutic targets. -
PPARγ/PPARδ Agonist
15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is an endogenous cyclopentenone prostaglandin that targets peroxisome proliferator-activated receptors, specifically acting as a selective agonist for PPARγ with an EC50 of 2 µM and a covalent agonist for PPARδ. This compound is known to facilitate the differentiation of C3H10T1/2 fibroblasts into adipocytes with an EC50 of 7 μM. Due to its effects on adipogenesis and metabolism, 15d-PGJ2 is utilized in research exploring obesity, diabetes, and metabolic syndrome pathways. -
PPARδ Agonist
Seladelpar sodium salt is a potent and selective agonist of the PPARδ receptor, demonstrating an EC50 of 2 nM. It exhibits more than 750-fold selectivity over PPARα and 2500-fold selectivity over PPARγ. This compound is primarily utilized in research regarding primary biliary cholangitis, contributing to the understanding of metabolic and inflammatory pathways. -
PPARγ Antagonist
SR1664 is a potent antagonist of peroxisome proliferator-activated receptor gamma (PPARγ). It effectively binds to PPARγ and inhibits Cdk5-mediated phosphorylation of the receptor, demonstrating an IC50 value of 80 nM and a Ki of 28.67 nM. This compound has valuable applications in research focused on metabolic regulation and the development of therapeutic strategies for conditions such as obesity and diabetes. -
PPARγ Activator
Convallatoxin is a PPARγ activator derived from the plant Adonis amurensis. It exhibits significant anti-inflammatory effects by mitigating colitic inflammation through the activation of PPARγ and the suppression of NF-κB signaling pathways. Additionally, Convallatoxin serves as a substrate for P-glycoprotein, identifying Val982 as a critical amino acid for its transport. This compound also enhances ligand-induced micro-opioid receptor (MOR) endocytosis, demonstrating high potency and efficacy, making it valuable for research in inflammation and cellular signaling. -
PPAR-γ Activator
Glabrone, a PPAR-γ activator derived from the roots of Glycyrrhiza glabra, demonstrates notable ligand binding activity to this nuclear receptor. In addition to its role as a specific probe substrate for UGT1A9, Glabrone's metabolites inhibit neuraminidase, thus preventing influenza virus release. This compound is suitable for research applications focused on herb-drug interactions and the evaluation of anti-influenza viral activity.
