Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PPAR agonist
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively. -
PPAR-δ agonist
Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist. -
PTP1B/IKK-βinhibitor and dual PPARα and PPARβ agonist
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ. -
PPARδ agonist
Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy. -
PPAR alpha/gamma agonist
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively. -
PPARγ agonist
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes. -
PPAR agonist
Indeglitazar is an orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma (γ). -
PPARγ agonist
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. -
dual α/γ PPAR activator
Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator. -
PPAR alpha agonist
Pemafibrate, also known as (R)-K 13675, is a PPAR alpha agonist. -
PPARγ agonist
Sipoglitazar, also known as TAK-654, is a PPARγ agonist potentially for the treatment of diabetes. -
MMP Inhibitor/PPARα Agonists
Auraptene is an orally active geranyloxycoumarin compound naturally found in plants of the *Brassicaceae* family. It exhibits a wide range of biological activities, including antibacterial, anti-pathogenic, antioxidant, anti-tumor, and neuroprotective effects. Auraptene has shown therapeutic potential in the management of various chronic conditions such as hypertension and cystic fibrosis, making it a valuable compound for pharmacological and nutraceutical research. -
PPAR agonist
Lobeglitazone sulfate is a novel thiazolidinedione and an orally active agonist of peroxisome proliferator-activated receptors (PPARs), with EC50 values of 137.4 nM for PPARγ and 546.3 nM for PPARα. It also acts as an inhibitor of the ERK/JNK/Smad/NF-κB signaling pathways. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic activities, supporting its potential in the treatment of metabolic and inflammatory diseases. -
EGFR/PI3K Inhibitor
MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia. -
PPAR agonist
Lobeglitazone is a novel thiazolidinedione-class compound and an orally active dual agonist of peroxisome proliferator-activated receptors (PPARs), with EC₅₀ values of 137.4 nM for PPARγ and 546.3 nM for PPARα. In addition to its metabolic effects, Lobeglitazone functions as an inhibitor of multiple pro-inflammatory and pro-fibrotic signaling pathways, including ERK, JNK, Smad, and NF-κB. Lobeglitazone exhibits a broad range of pharmacological activities, including anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic effects. These properties make it a promising candidate for therapeutic research in metabolic syndrome, type 2 diabetes, cardiovascular disease, and fibrosis-related conditions. -
PPARγ Agonist
Ciglitazone is a potent and selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), with an EC50 of 3 μM. It effectively inhibits the proliferation and differentiation of Th17 cells and serves as a hypoglycemic agent in obese-hyperglycemic animal models. Additionally, Ciglitazone promotes apoptosis through the activation of p38 MAPK and facilitates the nuclear translocation of apoptosis-inducing factor (AIF) in opossum kidney (OK) renal epithelial cells, making it a valuable tool for research in metabolic and renal diseases. -
RNA RIBOTAC Degrader
Dovitinib-RIBOTAC TFA is a targeted RNA RIBOTAC degrader that specifically binds to and degrades pre-miR-21. This compound demonstrates significant anti-tumor activity and effectively inhibits breast cancer metastasis. It serves as a valuable tool for research involving RNA-targeted degradation and its implications in cancer biology. -
PPAR Activator
Bilobetin acts as a PPARα activator, enhancing lipid metabolism and insulin sensitivity. It effectively reduces blood lipid levels by promoting hepatic lipid uptake and oxidation, while decreasing triglyceride secretion and accumulation in tissues. Additionally, Bilobetin stimulates the phosphorylation and nuclear translocation of PPARα, resulting in increased cAMP levels and PKA activity. This compound is significant for research in metabolic disorders, particularly those related to insulin resistance and lipid regulation. -
PPAR δ/γ Agonist
ZLY06 is a dual agonist of peroxisome proliferator-activated receptors (PPAR) δ and γ, exhibiting EC50 values of 341 nM and 237 nM, respectively. This compound promotes hepatic lipid accumulation through the inhibition of AKT1 phosphorylation, leading to the upregulation of CD36. Furthermore, ZLY06 enhances glucose and lipid metabolism while preventing weight gain, and mitigates fatty liver by facilitating β-oxidation of fatty acids and suppressing hepatic lipogenesis. It is valuable for research in metabolic disorders and fatty liver disease. -
PPARγ Activator
12-Nitrolinoleate is a potent peroxisome proliferator-activated receptor γ (PPARγ) activator derived from linoleic acid through nitration. It effectively induces PPARγ-dependent gene expression in MCF-7 cells, demonstrating an EC50 of 0.045 μM. Additionally, 12-Nitrolinoleate exhibits anti-inflammatory properties by inhibiting NF-κB transcription in RAW 264.7 cells, along with reducing levels of pro-inflammatory cytokines such as IL-6, TNF-α, and CCL2 in response to LPS stimulation. This compound is valuable for research applications focused on metabolic regulation and inflammation. -
PPARγ Agonist
Rosiglitazone hydrochloride is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), demonstrating an EC50 of 60 nM and a Kd of 40 nM. In addition to its primary action, it acts as a TRPC5 activator with an EC50 of 30 μM and a TRPM3 inhibitor. This compound is extensively utilized in research related to obesity, diabetes, cellular senescence, and ovarian cancer. -
PPARγ Agonist
Rosiglitazone potassium is a selective PPARγ agonist with an EC50 of 60 nM and a Kd of 40 nM. This compound also acts as a TRPC5 activator (EC50: 30 μM) while inhibiting TRPM3. It is utilized in research investigating obesity, diabetes, cellular senescence, and ovarian cancer. -
PPARγ Agonist
Pioglitazone potassium is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ), demonstrating high-affinity binding to the PPARγ ligand-binding domain with EC50 values of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. This compound is commonly utilized in diabetes research to explore its effects on insulin sensitivity and glucose metabolism. Its action on PPARγ makes it a valuable tool for studying metabolic disorders and related therapeutic interventions. -
Selective PPARγ Agonist
Pioglitazone-d4 is a deuterium-labeled derivative of Pioglitazone, a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). This compound demonstrates high affinity for the PPARγ ligand-binding domain, with EC50 values of 0.93 μM for human and 0.99 μM for mouse PPARγ. Pioglitazone-d4 is utilized in metabolic research to study insulin sensitivity, adipogenesis, and the mechanisms underlying type 2 diabetes mellitus. -
PPAR-α/γ and PPAR-γ Agonist
Dehydroabietic acid is a diterpene resin acid that serves as a dual agonist for PPAR-α and PPAR-γ, with partial agonist activity at PPAR-γ. This compound exhibits significant biological activities, including anti-bacterial, anti-fungal, anti-inflammatory, and anti-cancer effects. It has been shown to mitigate insulin resistance and hepatic steatosis induced by high-fat diet consumption in animal models, making it a valuable reagent for research in metabolic disorders and inflammatory diseases. -
PPAR Inhibitor
AZ0108 is a selective inhibitor of poly(ADP-ribose) polymerases (PARPs), including PARP1, PARP2, PARP3, PARP6, TNKS1, and TNKS2. It displays potent inhibitory activity with IC50 values of <0.03 μM for PARP1 and PARP2, and exhibits significant biological effects such as preventing centrosome clustering with an EC50 of 0.053 μM. Additionally, AZ0108 demonstrates cytotoxicity in OCI-LY-19 cells, with a GI50 value of 0.017 μM, and shows favorable pharmacokinetic properties in rat and mouse models, making it a valuable tool for cellular and molecular biology research focused on DNA repair and cancer therapeutic studies. -
PPAR-1 Inhibitor
AZD-9574-acid is a selective PPAR-1 inhibitor that serves as a crucial building block for the development of PROTAC molecules. Its inhibition of PPAR-1 demonstrates significant potential in the regulation of metabolic pathways and inflammatory responses. This compound is essential for researchers exploring targeted protein degradation and its applications in therapeutic development. -
PPAR Activator
Alpinetin is a flavonoid that acts as a PPAR-γ activator, demonstrating significant anti-inflammatory and hepatoprotective properties. It effectively inhibits lipopolysaccharide (LPS)-induced inflammation and protects against LPS-induced renal injury by modulating TLR4 expression and activating the Nrf2 pathway. Its diverse biological activities make Alpinetin a valuable reagent for research into tumor biology, cardiovascular health, and neuroprotection. -
Partial PPARγ Agonist
Oroxin A is a partial agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It enhances PPARγ transcriptional activity through binding to the PPARγ ligand-binding domain. Additionally, Oroxin A demonstrates inhibitory effects on α-glucosidase and possesses antioxidant properties. Its anti-breast cancer potential is attributed to the induction of endoplasmic reticulum stress-mediated cellular senescence, making it a valuable tool for research in metabolic and cancer biology. -
PPAR Activator
Angeloylgomisin H is a PPAR-γ activator derived from the lignin extract of Schisandra rubriflora. This compound has demonstrated the ability to enhance insulin-stimulated glucose uptake, making it a valuable candidate for research in metabolic disorders and diabetes. Its mechanism of action may provide insights into therapeutic strategies aimed at improving insulin sensitivity and glucose metabolism. -
PPARγ Agonist
Ankaflavin is an orally active peroxisome proliferator-activated receptor gamma (PPARγ) agonist, derived from Monascus-fermented red rice. This compound demonstrates selective cytotoxicity in cancer cells, inducing apoptosis and facilitating cell death. Additionally, Ankaflavin exhibits notable anti-inflammatory, anti-cancer, anti-atherosclerotic, and hypolipidemic properties, making it useful for various research applications in cancer biology and metabolic disorders. -
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 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 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.
