Catalog No.
Product Name
Application
Product Information
Citations
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PPARγ Agonist
BR101549 is a non-thiazolidinedione (non-TZD) agonist of peroxisome proliferator-activated receptor gamma (PPARγ). It demonstrates activation of PPARγ comparable to that of Pioglitazone in vitro. This compound has been shown to effectively regulate blood glucose levels in mouse models, making it a valuable tool for anti-diabetic research and studies related to metabolic disorders. -
PPARγ Agonist
PPARγ Agonist 16 acts as a selective agonist for peroxisome proliferator-activated receptor gamma (PPARγ), demonstrating competitive binding to the ligand-binding domain (LBD) with an IC50 of 1790 nM. This compound is notable for its ability to inhibit ear swelling in murine models and shows promising anti-hyperglycemic effects in streptozotocin-induced diabetes models. PPARγ Agonist 16 is valuable for research applications focused on metabolic disorders and inflammation. -
PPAR-γ Activator
Apo-12'-lycopenal is a metabolite of Lycopene acting as a PPAR-γ activator. It is known to enhance adipocyte differentiation and stimulate adiponectin secretion, making it of interest in studies related to metabolic regulation and obesity research. Its role in modulating PPAR-γ activity positions it as a valuable tool for investigating lipid metabolism and insulin sensitivity. -
PPARγ Agonist
AMG131 benzenesulfonate is a selective peroxisome proliferator-activated receptor γ (PPARγ) agonist, classified as a non-thiazolidinedione (TZD) modulator. It binds to the PPARγ receptor, occupying a unique position in the binding pocket, which allows for distinct interactions compared to traditional TZDs. This compound has demonstrated potential in research pertaining to the treatment of type-2 diabetes mellitus, making it a valuable tool for investigating PPARγ-related metabolic pathways. -
PPARγ Agonist
PPARγ agonist 8 is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It effectively induces peroxisome proliferator response element (PPRE)-luciferase activity with an EC50 of 0.2 μM, highlighting its potency in modulating PPARγ signaling pathways. This compound is valuable for studying the role of PPARγ in metabolic regulation, insulin sensitivity, and inflammation-related research. -
PPARγ Agonist
DS-6930 is a potent and selective agonist of PPARγ, exhibiting an EC50 of 41 nM. This compound significantly reduces plasma glucose levels while exhibiting fewer PPARγ-related adverse effects compared to traditional agents. DS-6930 is utilized for research in diabetes and metabolic disorders, making it a valuable tool for exploring therapeutic strategies in these areas. -
PPAR Agonist
Reglitazar is a selective agonist for peroxisome proliferator-activated receptors α and β (PPAR α and PPAR β). It is known to enhance insulin sensitivity, reduce blood glucose levels, and regulate lipid metabolism. This compound is useful in research applications focused on metabolic disorders, diabetes, and cardiovascular diseases, providing insights into the modulation of metabolic pathways. -
PPAR Agonist
MHY 553 is a PPARα agonist that enhances fatty acid oxidation and reduces liver fat accumulation. This compound has demonstrated efficacy in mitigating triglyceride accumulation induced by liver X receptor agonists in HepG2 cells. Additionally, MHY 553 significantly suppresses inflammatory mRNA expression in aging rats, making it a valuable tool for research on metabolic disorders and age-related inflammation. -
PPARα/γ Activator
GW-9820 is a potent activator of both PPARα and PPARγ, exhibiting EC50 values of 0.37 μM and 0.288 μM, respectively. This compound has been shown to enhance the expression of CLA-1, a key player in lipid metabolism and inflammation. GW-9820 is primarily utilized in research focused on atherosclerosis, offering insights into the modulation of metabolic pathways linked to cardiovascular diseases. -
PPARα Agonist
KRP-105 is a selective agonist of peroxisome proliferator-activated receptor alpha (PPARα), exhibiting an effective concentration (EC50) of 8 nM. This compound has demonstrated the ability to significantly lower serum levels of triglycerides, total cholesterol, and non-high-density lipoprotein cholesterol. KRP-105 is suitable for research applications focused on metabolic diseases, particularly dyslipidemia. -
PPAR Modulator
SR2595 is an inverse agonist of peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting an IC50 value of 30 nM. This compound functions by modulating PPARγ activity, leading to alterations in gene expression associated with lipid metabolism and insulin sensitivity. SR2595 is primarily used in research related to metabolic disorders, obesity, and diabetes, making it a valuable tool for studying PPARγ signaling pathways and their implications in various physiological processes. -
PPARγ ligand
SR 1824 is a non-agonist ligand for peroxisome proliferator-activated receptor gamma (PPARγ), functioning primarily by inhibiting Cdk5-mediated phosphorylation. This compound exhibits anti-diabetic properties, making it a valuable tool for research focused on metabolic disorders and the modulation of PPARγ signaling pathways. Its unique mechanism supports investigations into the regulation of insulin sensitivity and the therapeutic potential in diabetes-related studies. -
COX-2 Inhibitor/PPAR-γ Activator
Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury. -
LTD4 Antagonist/PPAR-γ Agonist
LTD4 antagonist 3 (FK011 hydrochloride) is a selective leukotriene D4 (LTD4) antagonist that also exhibits agonistic activity for peroxisome proliferator-activated receptor gamma (PPAR-γ). This compound demonstrates enhanced PPAR-γ activation with a fold-increase of 1.50 at 1 μM and 2.35 at 10 μM. LTD4 antagonist 3 is valuable for research in the development of non-steroidal anti-inflammatory drugs (NSAIDs) and related therapeutic applications targeting inflammatory pathways. -
PPAR Modulator
C333H is a selective modulator of PPARγ, effectively exhibiting insulin-sensitizing and hypoglycemic properties. In diabetic mouse models, C333H demonstrates insulin-sensitizing effects comparable to thiazolidinediones without causing significant weight gain or increased adipose tissue mass. The compound elevates levels of high molecular weight adiponectin isoforms in diabetic db/db mice and reduces serine phosphorylation of PPARγ at residue 273 in brown adipose tissue, selectively modulating the expression of specific target genes in adipose tissue. Additionally, C333H shows weak recruitment of co-activators and weak dissociation of co-repressors in vitro, indicating its potential as an inhibitor of type 2 diabetes. -
PPARδ Agonist
PPARδ Agonist 10 is a selective, orally active partial agonist targeting peroxisome proliferator-activated receptor delta (PPARδ) with EC50 values of 0.053 μM for human PPARδ (LBD) and 0.30 μM for mouse PPARδ. This compound exhibits full agonistic activity on free fatty acid oxidation in muscle cells, both in vitro and in vivo, while displaying partial agonism in transactivation assays. PPARδ Agonist 10 is suitable for research focused on dyslipidemia and metabolic disorders. -
PPARγ Modulator
PPARγ modulator-1 is a non-agonistic modulator of the peroxisome proliferator-activated receptor gamma (PPARγ). It exhibits high binding affinity for PPARγ and inhibits kinase-mediated phosphorylation of this receptor. This compound is suitable for research applications focused on metabolic diseases, providing a means to study the effects of PPARγ modulation while potentially minimizing side effects associated with traditional agonists. -
PPARδ Agonist
L-783483 is a potent agonist of Peroxisome Proliferator-Activated Receptor delta (PPARδ). This compound has demonstrated the ability to reduce inflammation, as evidenced by its efficacy in attenuating Carrageenan-induced paw edema in murine models. L-783483 is useful in studies exploring metabolic disorders, inflammatory responses, and the therapeutic potential of PPARδ activation. -
PPARδ Agonist
PPARδ Agonist 11 is a selective agonist for peroxisome proliferator-activated receptor delta (PPARδ), exhibiting an EC50 of 20 nM. This compound effectively reduces nitrite oxide levels and pro-inflammatory cytokines, such as TNFα and IL-6, in LPS-stimulated RAW264.7 cells, demonstrating its anti-inflammatory activity through the NF-κB pathway. Additionally, PPARδ Agonist 11 shows good stability in human liver microsomes and plasma, and it alleviates Carrageenan-induced foot edema, making it a valuable tool for research in inflammation and metabolic disorders. -
PPARα/γ dual agonist
MHY908 is a potent dual agonist of peroxisome proliferator-activated receptors alpha (PPARα) and gamma (PPARγ). This compound enhances lipid metabolism and insulin sensitivity, making it a valuable tool in research related to metabolic disorders and obesity. Additionally, MHY908 inhibits melanogenesis by reducing the activity of mushroom tyrosinase, which may have implications in studies of pigmentation and skin biology. -
PPAR Modulator
CRX000227 is a PPAR modulator that selectively influences peroxisome proliferator-activated receptors (PPARs), playing a significant role in metabolic regulation. This compound demonstrates potential in the study of metabolic disorders and cell proliferation activities, making it a valuable tool for investigating the underlying mechanisms of various diseases related to metabolic dysfunction. Its utility in research applications may aid in the development of therapeutic strategies targeting metabolic and proliferative disorders. -
PPARγ Partial Agonist
PPARγ Agonist 2 is a potent partial agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). This compound demonstrates significant biological activity in modulating glucose and lipid metabolism, making it an essential tool for studying metabolic diseases. It is particularly useful in research applications focused on obesity, diabetes, and cardiovascular disorders. -
PPAR Agonist
PPARα/δ Agonist 3 is a selective agonist targeting peroxisome proliferator-activated receptors (PPARs), specifically activating PPARα, PPARδ, and PPARγ with EC50 values of 5.6 nM, 3.4 nM, and 1278 nM, respectively. This compound demonstrates significant anticholestatic activity in mouse models of cholestatic liver disease induced by ANIT or CDCA. It is useful for studying the role of PPAR activation in lipid metabolism and the pathophysiology of liver diseases. -
PPARγ Agonist
PPARγ agonist-22 is a selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ), which plays a crucial role in regulating glucose and lipid metabolism. This compound enhances cellular glucose uptake and decreases lipid accumulation in adipocytes, making it valuable in investigating metabolic disorders. PPARγ agonist-22 is particularly relevant for studies focused on the pathophysiology and treatment of type 2 diabetes. -
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 Inhibitor, heme oxygenase-1 Activator, Nrf2 Activator
PIISVYWK is a potent PPARγ inhibitor that also acts as an activator of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2). This compound effectively modulates the HO-1/Nrf2 signaling pathway, contributing to the reduction of oxidative stress and inflammation, while also exhibiting anti-obesity properties. PIISVYWK is suitable for research applications focused on obesity and related metabolic disorders. -
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. - Fenofibrate is a drug of the fibrate class. It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease.
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PPARγ agonist
5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
