PPAR

Cat. No.

A11437

CAS No.

317318-70-0

GW 501516

Synonyms: GW1516; GSK-516

GW501516 (GW1516 or GSK-516) is a drug that acts as a PPARδ modulator.

Cat. No.

A16309

CAS No.

1361504-77-9

DG172 dihydrochloride

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.

Cat. No.

A19031

CAS No.

2095128-17-7

MA-0204

MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).

Cat. No.

A19493

CAS No.

1010412-80-2

GSK376501A

GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.

Cat. No.

A35979

CAS No.

921195-93-9

GED 0507-34-Levo

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.

Cat. No.

A38260

CAS No.

1830320-32-5

RB394

RB394 is a potent dual soluble epoxide hydrolase (sEH) and peroxisome proliferator-activated receptor gamma (PPARγ) modulator. This compound promotes adipocyte browning and demonstrates significant cardioprotective effects. RB394 is an invaluable tool for researchers studying metabolic syndrome and related metabolic disorders.

Cat. No.

A39909

CAS No.

2924573-90-8

FX-909

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.

Cat. No.

A39921

CAS No.

315224-26-1

AMG131

Synonyms: INT131

AMG131 is a selective peroxisome proliferator-activated receptor γ (PPARγ) modulator, functioning as a potent non-thiazolidinedione (TZD) agonist. It binds to PPARγ in the same pocket as TZDs, yet interacts with the receptor at unique contact points, potentially leading to differential biological effects. This compound has significant potential for research applications related to type-2 diabetes mellitus and metabolic disorders.

Cat. No.

A39922

CAS No.

2095128-20-2

Bocidelpar

Synonyms: ASP0367; MA-0211

Bocidelpar is a selective PPAR-δ modulator that activates the PPAR-δ downstream signaling pathway, leading to the upregulation of target genes such as ABCA1 and ACAA2. This compound promotes fatty acid oxidation and enhances mitochondrial biogenesis, ultimately improving mitochondrial dysfunction. Bocidelpar is particularly useful in researching diseases associated with mitochondrial dysfunction, including primary mitochondrial myopathy (PMM) and Duchenne muscular dystrophy (DMD).

Cat. No.

A39938

CAS No.

423150-91-8

BAY-4931

BAY-4931 is a selective inverse agonist of PPARγ, exhibiting potent action with an IC50 of 0.17 nM. This compound effectively modulates PPARγ activity, making it a valuable tool for investigating metabolic disorders and insulin sensitivity. Its unique mechanism of action allows for detailed studies of PPARγ's role in various biological processes and therapeutic applications.

Cat. No.

A39939

CAS No.

1356497-91-0

ST247

ST247 is a potent inverse agonist of the peroxisome proliferator-activated receptor beta/delta (PPARβ/δ). It exhibits a high affinity for this target and modulates the expression of the activation marker CCL2 in a manner contrary to typical agonist activity. ST247 effectively promotes the interaction with corepressors and inhibits agonist-induced transcriptional activity of PPARβ/δ. This compound is valuable for research into metabolic disorders and inflammation, offering insights into the regulatory mechanisms mediated by PPARβ/δ.

Cat. No.

A39953

CAS No.

193012-35-0

FK614

FK614 is a selective PPARγ modulator (SPPARM) that functions as a PPARγ agonist with significant anti-diabetic properties. This compound exhibits distinct effects on PPARγ activation throughout various stages of adipocyte differentiation. FK614 is utilized in research focused on hyperglycemia, hypertriglyceridemia, glucose intolerance, and type 2 diabetes, making it a valuable tool for understanding metabolic disorders.

Cat. No.

A39960

CAS No.

2891706-79-7

BAY-5516

BAY-5516 is an inverse agonist of PPARG, exhibiting an IC50 value of 6.1 ± 3.6 nM. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research into cancer therapeutics. It is suitable for studies focusing on the modulation of PPARG signaling pathways and their implications in various tumor models.

Cat. No.

A39978

CAS No.

1415321-64-0

SR10221

SR10221 is a noncovalent inverse agonist of peroxisome proliferator-activated receptor gamma (PPARγ). This compound exhibits significant biological activity by repressing downstream PPARγ target genes, which contributes to growth inhibition in bladder cancer cell lines. SR10221 is primarily utilized in research applications aimed at understanding PPARγ signaling pathways and developing potential therapeutic strategies for bladder cancer.

Cat. No.

A39989

CAS No.

420826-65-9

BAY-0069

BAY-0069 is a selective inverse agonist of PPARγ, exhibiting potent inhibition with IC50 values of 6.3 nM for human PPARγ and 24 nM for mouse PPARγ. This compound serves as a valuable tool for investigating the roles of PPARγ in cancer research, providing insights into its regulatory mechanisms in tumorigenesis and potential therapeutic strategies. Its high selectivity enhances its utility in experimental settings.

Cat. No.

A40010

CAS No.

2891706-78-6

BAY-5094

BAY-5094 is an inverse agonist of the peroxisome proliferator-activated receptor gamma (PPARG). This compound exhibits oral bioactivity and has potential applications in the study of luminal bladder cancer. Its mode of action allows for investigation into the role of PPARG in tumorigenesis and cancer progression.

Cat. No.

A40064

CAS No.

95520-87-9

PA-082

PA-082 is a selective modulator of peroxisome proliferator-activated receptor gamma (PPAR-γ) functioning as a partial agonist. It promotes the partial recruitment of coactivators SRC1, TIF2, and SRC3, while fully recruiting PGC1-α to the PPAR-γ ligand-binding domain. PA-082 effectively inhibits triglyceride accumulation during de novo adipogenesis and counteracts lipid buildup induced by Rosiglitazone. Furthermore, this compound enhances insulin-stimulated glucose uptake in adipocytes and provides protection against TNFα-induced insulin resistance, making it a valuable tool for research into type 2 diabetes.

Cat. No.

A40076

CAS No.

2089159-00-0

PPARγ/δ modulator 1

PPARγ/δ modulator 1 is a selective modulator of the peroxisome proliferator-activated receptors (PPARs), acting as an antagonist for PPARδ and a partial agonist for PPARγ. It exhibits Ki values of 14.4 nM for PPARδ and 5.31 μM for PPARγ, indicating strong binding affinity. This compound demonstrates biological activities with an EC50 of 7.3 μM for PPARδ corepression and 12.6 μM for the stimulation of adiponectin production. Its modulation capabilities make it a valuable tool for research on metabolic disorders and related pathways.

Cat. No.

A40092

CAS No.

2891706-83-3

BAY-9683

BAY-9683 is an orally active covalent inverse agonist of PPARG (Peroxisome Proliferator-Activated Receptor Gamma). It effectively inhibits the activity of overactive PPARG, making it a valuable tool for investigating diseases associated with PPARG dysregulation, including luminal bladder cancer. This compound is suitable for research applications focused on metabolic regulation and cancer biology.

Cat. No.

A40101

CAS No.

2982533-42-4

SP-C01

SP-C01 is a potent modulator targeting soluble epoxide hydrolase (sEH) and serving as a partial agonist of peroxisome proliferator-activated receptor gamma (PPARγ). This compound exhibits significant inhibitory effects on Ser273 phosphorylation, highlighting its potential role in metabolic research and the modulation of inflammatory pathways. SP-C01 is suitable for studies investigating the therapeutic effects on metabolic disorders and the regulation of lipid metabolism.

Cat. No.

A40122

CAS No.

1415252-61-7

SR2595

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.

Cat. No.

A40126

CAS No.

870095-15-1

C333H

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.

Cat. No.

A40129

CAS No.

1415321-54-8

PPARγ modulator-1

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.

Cat. No.

A40133

CAS No.

686769-92-6

CRX000227

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.

Cat. No.

A40154

CAS No.

2835447-74-8

YGT-31

YGT-31 is a selective modulator of peroxisome proliferator-activated receptor gamma (PPARγ) with an IC50 of 1.72 μM and a Ki of 0.62 μM. This compound has demonstrated the ability to lower blood glucose levels and enhance insulin sensitivity in db/db mouse models of type 2 diabetes by inhibiting CDK5-mediated phosphorylation at Ser273 of PPARγ. Additionally, YGT-31 exhibits protective effects against hepatic steatosis in non-alcoholic fatty liver disease (NAFLD) models, highlighting its potential in metabolic disease research.