- Cat. No.
- A11437
GW 501516
Synonyms: GW1516; GSK-516
GW501516 (GW1516 or GSK-516) is a drug that acts as a PPARδ modulator.
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- Cat. No.
- A19031
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).
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- Cat. No.
- A19493
GSK376501A
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
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- Cat. No.
- A35979
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.
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- Cat. No.
- A38260
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.
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- Cat. No.
- A39921
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.
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- Cat. No.
- A39922
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).
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- Cat. No.
- A39953
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.
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- Cat. No.
- A40018
E17241
E17241 is an inducer of ATP-binding cassette transporter A1 (ABCA1) that significantly enhances ABCA1 protein levels in RAW 264.7 macrophages. It also acts as an agonist for peroxisome proliferator-activated receptors (PPARs), contributing to metabolic regulation. Notably, E17241 has demonstrated the capability to reduce plasma glucose levels and body weight in KKAy diabetic mice subjected to a high-fat and high-glucose diet, making it a valuable reagent for research on lipid metabolism and diabetes management.
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- Cat. No.
- A40064
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.
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- Cat. No.
- A40076
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.
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- Cat. No.
- A40101
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.
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- Cat. No.
- A40126
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.
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- Cat. No.
- A40129
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.
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- Cat. No.
- A40133
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.
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- Cat. No.
- A40154
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.
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- Cat. No.
- A40162
PPARγ modulator-2
PPARγ modulator-2 is a reversible modulator of the peroxisome proliferator-activated receptor gamma (PPARγ), targeting its ligand-binding domain with an IC50 of 41 nM. This compound demonstrates significant biological activity by reducing blood glucose levels and enhancing glucose and insulin tolerance. Its efficacy has been validated in db/db mouse models, highlighting its potential applications in diabetes research and metabolic disorders.
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- Cat. No.
- A40204
PPARα-MO-1
PPARα-MO-1 is a potent modulator of peroxisome proliferator-activated receptor alpha (PPARα), contributing to lipid metabolism and glucose homeostasis. This compound has potential applications in the study of metabolic disorders, including obesity and type 2 diabetes, by regulating gene expression involved in fatty acid oxidation and inflammation. It serves as an important tool for researchers investigating the role of PPARα in metabolic pathways and therapeutic strategies.
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