- Cat. No.
- A12413
GW6471
GW6471 is a PPARα antagonist, shown to completely inhibit GW409544-induced activation of PPARα.
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PPAR agonists and antagonists target peroxisome proliferator-activated receptors (PPARs), a nuclear receptor family. The first PPAR was identified in 1990 as a member of the steroid hormone receptor superfamily activated by peroxisome proliferators. The three subtypes, PPARα, PPARδ and PPARγ, act as ligand-activated transcription factors in tissues such as liver, muscle and fat. PPARγ promotes adipocyte differentiation, and thiazolidinediones were shown in 1995 to bind it with high affinity. Examples include rosiglitazone and troglitazone for PPARγ, fenofibrate for PPARα and GW 501516 for PPARδ. Elafibranor acts on PPARα and PPARδ, while T0070907 is a PPARγ antagonist for blocking studies.
GW6471 is a PPARα antagonist, shown to completely inhibit GW409544-induced activation of PPARα.
Synonyms: GW1516; GSK-516
GW501516 (GW1516 or GSK-516) is a drug that acts as a PPARδ modulator.
T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2.
GW 9662 is a selective PPARγ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively).
GSK-3787 is a potent and selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pIC50 = 6.6).
GSK 0660 is a selective PPARβ antagonist (IC50 values are 0.155, > 10 and ??? 10 μM at PPARβ, PPARα and PPARγ respectively).
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.
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.
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.
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively.
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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).
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
Synonyms: NID 525
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 µM.
Synonyms: BMS 426707-01 racemate; BMS-426707-01
Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator.
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.
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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.
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.
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.
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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.
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.
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.
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.
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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.
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.