- Cat. No.
- A12413
GW6471
GW6471 is a PPARα antagonist, shown to completely inhibit GW409544-induced activation of PPARα.
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- Cat. No.
- A11588
T0070907
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.
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- Cat. No.
- A11984
GW 9662
GW 9662 is a selective PPARγ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively).
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- Cat. No.
- A12391
GSK-3787
GSK-3787 is a potent and selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pIC50 = 6.6).
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- Cat. No.
- A12392
GSK 0660
GSK 0660 is a selective PPARβ antagonist (IC50 values are 0.155, > 10 and ??? 10 μM at PPARβ, PPARα and PPARγ respectively).
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- Cat. No.
- A15651
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.
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- Cat. No.
- A15680
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.
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- Cat. No.
- A15707
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.
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- Cat. No.
- A18771
NXT629
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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- Cat. No.
- A19926
RG-12525
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.
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- Cat. No.
- A21411
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.
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- Cat. No.
- A26090
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.
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- Cat. No.
- A39730
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.
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- Cat. No.
- A39914
SR1664
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.
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- Cat. No.
- A39915
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.
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- Cat. No.
- A39916
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.
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- Cat. No.
- A39918
(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.
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- Cat. No.
- A39920
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.
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- Cat. No.
- A39926
Mifobate
Synonyms: SR-202
Mifobate is a potent antagonist of peroxisome proliferator-activated receptor gamma (PPARγ), selectively inhibiting thiazolidinedione (TZD)-induced transcriptional activity with an IC50 of 140 μM. This compound does not affect the basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate demonstrates significant antiobesity and antidiabetic effects, making it valuable for research applications aimed at exploring metabolic disorders and therapeutic interventions for related conditions.
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- Cat. No.
- A39935
(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.
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- Cat. No.
- A39951
H-Trp-Glu-OH
Synonyms: G3335
H-Trp-Glu-OH is a selective and reversible antagonist of peroxisome proliferator-activated receptor gamma (PPARγ), with a dissociation constant (Kd) of approximately 8 µM. This compound has demonstrated cell permeability and presents potential as a lead compound in diabetes research. Its role in modulating PPARγ activity makes it an important tool for studying metabolic disorders and associated therapeutic pathways.
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- Cat. No.
- A39955
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.
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- Cat. No.
- A39964
8(S)-HETE
Synonyms: 8(S)-Hydroxyeicosatetraenoic acid
8(S)-HETE (8(S)-Hydroxyeicosatetraenoic acid) primarily acts as a PPARα activator, with demonstrated biological activity in stimulating mouse keratinocyte protein kinase C at an IC50 of 100 μM. This compound selectively activates PPARα at concentrations as low as 0.3 μM, making it valuable for research into skin biology and inflammatory responses. The stereochemical assignment of the (S) enantiomer is confirmed through chiral HPLC retention time comparisons with established data.
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- Cat. No.
- A39968
Amezalpat
Synonyms: TPST-1120
Amezalpat is a selective antagonist of PPARα, exhibiting an IC50 value of 58 nM. This compound demonstrates notable antineoplastic activity, making it a valuable tool for research in cancer biology and therapeutic applications targeting metabolic regulation and lipid homeostasis. Its use in scientific studies may help elucidate the role of PPARα in tumor progression and treatment resistance.
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