PPAR

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.

15 Items

  • Octocrylene
    Cat. No.
    A11900

    Octocrylene

    Octocrylene is an organic ultraviolet (UV) filter primarily known for absorbing UVB radiation and shorter UVA wavelengths. This compound acts as a partial agonist of PPARγ, influencing the transcription profiles of lipid metabolism enzymes. Additionally, Octocrylene exhibits cytotoxic and genotoxic effects on human skin fibroblasts and has been shown to mediate the biosynthesis of estrogens, such as estriol, in zebrafish larvae while impacting antioxidant pathways, including glutathione transferase and peroxisomes. Its applications include studies in photoprotection, environmental toxicology, and endocrine disruption research.

    500 mg
    $20.00
    1 g
    $25.00
    All 4 sizes
  • Balaglitazone
    Cat. No.
    A15013

    Balaglitazone

    Synonyms: DRF-2593; NN-2344

    Balaglitazone is a novel partial agonist of PPAR-gamma (γ).

    1 mg
    $75.00
    5 mg
    $185.00
    All 6 sizes
  • Oroxin A
    Cat. No.
    A15695

    Oroxin A

    Oroxin A is a partial agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It enhances PPARγ transcriptional activity through binding to the PPARγ ligand-binding domain. Additionally, Oroxin A demonstrates inhibitory effects on α-glucosidase and possesses antioxidant properties. Its anti-breast cancer potential is attributed to the induction of endoplasmic reticulum stress-mediated cellular senescence, making it a valuable tool for research in metabolic and cancer biology.

    1 mg
    $30.00
    5 mg
    $65.00
    All 7 sizes
  • Arhalofenate
    Cat. No.
    A21135

    Arhalofenate

    Synonyms: MBX 102; JNJ 39659100

    Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.

    1 mg
    $125.00
    5 mg
    $295.00
    All 8 sizes
  • GQ-16
    Cat. No.
    A39991

    GQ-16

    GQ-16 is an orally active partial agonist of PPARγ, exhibiting an IC50 of 1.84 μM and a Ki of 160 nM against human PPARγ. This compound effectively inhibits Cdk5-mediated Ser-273 phosphorylation, enhancing insulin sensitivity and glucose tolerance in obese and diabetic mouse models. Additionally, GQ-16 demonstrates cytotoxic effects against various tumor cell lines, making it a valuable reagent for research on obesity, diabetes, and cancer.

    5 mg
    $20.00
    10 mg
    $30.00
    All 7 sizes
  • E17241
    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.

    100 mg
    $940.00
    All 1 sizes
  • MBX-102 acid
    Cat. No.
    A40052

    MBX-102 acid

    MBX-102 acid is a selective partial agonist of PPAR-γ (Peroxisome Proliferator-Activated Receptor Gamma). This compound exhibits strong binding to plasma proteins, primarily serum albumin, which may influence its pharmacokinetics. MBX-102 acid is primarily utilized in research related to type 2 diabetes, aiding in the exploration of its role in glucose metabolism and insulin sensitivity.

    Out of stock

    All 3 sizes
  • Caulophyllogenin
    Cat. No.
    A40063

    Caulophyllogenin

    Caulophyllogenin is a triterpene saponin that acts as a partial agonist of PPARγ, exhibiting an EC50 of 12.6 μM. This compound plays a significant role in the modulation of glucose metabolism and adipogenesis, making it relevant for research on type-2 diabetes, obesity, metabolic syndrome, and inflammation. Its distinct biological activity allows for further exploration in the development of therapeutic strategies targeting metabolic disorders.

    1 mg
    $90.00
    5 mg
    $220.00
    All 4 sizes
  • Neoambrosin
    Cat. No.
    A40069

    Neoambrosin

    Neoambrosin is a sesquiterpene lactone that acts as a partial agonist of the PPARγ and TRPA1 receptors. This compound demonstrates potential biological activity related to hypoglycemia, analgesia, anti-inflammatory responses, and anticancer effects. Neoambrosin is suitable for research applications aimed at exploring metabolic disorders and pain management, as well as studying its role in inflammation and cancer therapeutics.

    Out of stock

    All 3 sizes
  • GSK-7227
    Cat. No.
    A40079

    GSK-7227

    GSK-7227 is a partial agonist of the peroxisome proliferator-activated receptor delta (PPARδ). It effectively regulates the expression of target genes associated with lipid metabolism, specifically CPT1a and PDK4, in skeletal muscle cells. This compound holds potential for studies focused on metabolic disorders and mitochondrial function modulation.

    1 mg
    $235.00
    5 mg
    $590.00
    All 6 sizes
  • GSK 1997132B
    Cat. No.
    A40085

    GSK 1997132B

    GSK 1997132B is a benzimidazole-derived partial agonist of PPARγ, notable for its ability to cross the blood-brain barrier with a pEC50 value of 8.0. This compound selectively activates PPARγ while exhibiting minimal activity on PPARα and PPARδ, addressing issues related to high blood clearance rates seen in earlier agents. GSK 1997132B is particularly relevant for research into Alzheimer's disease, providing a potential pathway for exploring therapeutic strategies that mitigate associated side effects such as weight gain and edema.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • PPARδ agonist 10
    Cat. No.
    A40127

    PPARδ agonist 10

    PPARδ Agonist 10 is a selective, orally active partial agonist targeting peroxisome proliferator-activated receptor delta (PPARδ) with EC50 values of 0.053 μM for human PPARδ (LBD) and 0.30 μM for mouse PPARδ. This compound exhibits full agonistic activity on free fatty acid oxidation in muscle cells, both in vitro and in vivo, while displaying partial agonism in transactivation assays. PPARδ Agonist 10 is suitable for research focused on dyslipidemia and metabolic disorders.

    1 mg
    $100.00
    5 mg
    $310.00
    All 3 sizes
  • PPARγ agonist 2
    Cat. No.
    A40134

    PPARγ agonist 2

    PPARγ Agonist 2 is a potent partial agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). This compound demonstrates significant biological activity in modulating glucose and lipid metabolism, making it an essential tool for studying metabolic diseases. It is particularly useful in research applications focused on obesity, diabetes, and cardiovascular disorders.

    Out of stock

    All 3 sizes
  • GW0072
    Cat. No.
    A40142

    GW0072

    GW0072 is a partial agonist of peroxisome proliferator-activated receptor gamma (PPARγ), selectively inducing transcriptional activity without directly binding to the receptor's AF-2 helix. This unique mechanism allows for specific modulation of PPARγ activity and may influence pathways related to metabolism and inflammation. GW0072 is valuable for research investigating obesity, diabetes, and metabolic syndrome, as well as studying the broader roles of PPARγ in cellular regulation and differentiation.

    25 mg
    $1,665.00
    All 1 sizes
  • (+)-Arhalofenate
    Cat. No.
    A40173

    (+)-Arhalofenate ((+)-MBX 102, (+)-JNJ 39659100)

    Synonyms: (+)-MBX 102; (+)-JNJ 39659100

    (+)-Arhalofenate is the less active enantiomer of Arhalofenate, a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ. This compound's primary mechanism involves modulating glucose metabolism and insulin sensitivity. It is primarily utilized in research focused on diabetes and metabolic disorders, contributing to the understanding of PPAR-γ's role in these physiological processes.

    1 mg
    $40.00
    5 mg
    $170.00
    All 6 sizes

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