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.

A15651

CAS No.

36052-37-6

Alpinetin

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.

Cat. No.

A15680

CAS No.

521-32-4

Bilobetin

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.

Cat. No.

A15707

CAS No.

66056-22-2

Angeloylgomisin H

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.

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.

A21411

CAS No.

331744-72-0

Peliglitazar racemate

Synonyms: BMS 426707-01 racemate; BMS-426707-01

Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator.

Cat. No.

A26090

CAS No.

774603-05-3

12-Nitrolinoleate

Synonyms: 12-Nitro-9-cis,12-cis-octadecadienoic acid

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.

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.

A39730

CAS No.

316371-83-2

Rosiglitazone sodium

Synonyms: BRL 49653 sodium

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.

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.

A39915

CAS No.

508-75-8

Convallatoxin

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.

Cat. No.

A39916

CAS No.

60008-02-8

Glabrone

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.

Cat. No.

A39918

CAS No.

29623-28-7

(S)-Coriolic acid

Synonyms: 13(S)-HODE

(S)-Coriolic acid is a potent PPARγ activator formed through the metabolism of linoleic acid by 15-lipoxygenase (15-LOX). This compound serves as a crucial intracellular signaling agent, influencing cell proliferation and differentiation across diverse biological systems. Additionally, (S)-Coriolic acid is known to induce mitochondrial dysfunction and contribute to airway epithelial injury, making it relevant for studies investigating cellular stress responses and respiratory health.

Cat. No.

A39920

CAS No.

59403-52-0

SDPC

Synonyms: PC(18:0/22:6); DHA-PC; 1-Stearoyl-2-docosahexaenoyl-sn-glyerco-3-phosphocholine

SDPC (DHA-PC) is a PPARγ activator that demonstrates significant anti-angiogenic properties. This phospholipid, featuring an ester bond with docosahexaenoic acid (DHA) at the sn-2 position, effectively inhibits the proliferation, migration, and tube formation of human umbilical vein endothelial cells. SDPC holds potential for applications in anti-tumor angiogenesis research, making it a valuable tool for studying tumor progression and vascular growth inhibition.

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.

A39935

CAS No.

2420-56-6

(10E,12Z)-Octadeca-10,12-dienoic acid

Synonyms: trans-10,cis-12 CLA2

(10E,12Z)-Octadeca-10,12-dienoic acid is a potent PPARα activator that plays a critical role in regulating lipid metabolism and adipocyte differentiation. This compound has demonstrated various biological activities, including antioxidant and antitumor effects, alongside the induction of proinflammatory cytokines and chemokines, which may contribute to decreased adipogenesis and insulin resistance. (10E,12Z)-Octadeca-10,12-dienoic acid also influences milk fat synthesis by reducing the expression of lipogenic enzymes and inhibiting fatty acid desaturation. Additionally, it has been shown to modulate lipoprotein lipase activity in cultured adipocytes and alter hepatic stearoyl-CoA desaturase expression in vivo.

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.

A39955

CAS No.

2921-20-2

2-(Tetradecylthio)acetic acid

2-(Tetradecylthio)acetic acid is a pan-peroxisome proliferator-activated receptor (pan-PPAR) activator. This compound is known to induce hypolipidemia by reducing plasma lipid levels and enhancing hepatic fatty acid oxidation in rodent models. Additionally, it increases the expression of genes associated with fatty acid uptake, activation, accumulation, and oxidation, making it a valuable tool for research on lipid metabolism and related 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.