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.

A11900

CAS No.

6197-30-4

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.

Cat. No.

A15013

CAS No.

199113-98-9

Balaglitazone

Synonyms: DRF-2593; NN-2344

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

Cat. No.

A15695

CAS No.

57396-78-8

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.

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.

A21135

CAS No.

24136-23-0

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.

Cat. No.

A31673

CAS No.

292615-75-9

CAY10506

CAY10506 is a potent ligand of peroxisome proliferator-activated receptor gamma (PPARγ) that induces cell death and reactive oxygen species (ROS) production through a PPARγ-dependent mechanism. This compound demonstrates radiosensitizing properties, enhancing apoptosis induced by gamma radiation and facilitating caspase-3-mediated cleavage of poly (ADP-ribose) polymerase (PARP). CAY10506 is applicable in cancer research, particularly in studies focused on PPARγ signaling pathways and radiation therapy augmentation.

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.

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.

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.

A39974

CAS No.

862901-87-9

LT175

LT175 is a dual ligand targeting peroxisome proliferator-activated receptors alpha and gamma (PPARα/γ). As an orally active partial agonist, it exhibits effective receptor affinity with EC50 values of 0.22 μM for hPPARα, 0.26 μM for mPPARα, and 0.48 μM for hPPARγ. LT175 modulates coregulator recruitment, specifically cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1), via interaction in the hydrophobic "diphenyl pocket" of PPARγ. This compound demonstrates significant insulin-sensitizing effects while reducing adipogenic activity, making it valuable for research in metabolic disorders.

Cat. No.

A39991

CAS No.

870554-67-9

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.

Cat. No.

A40011

CAS No.

66056-18-6

Glycyrin

Glycyrin is a potent ligand for the peroxisome proliferator-activated receptor gamma (PPAR-γ). This compound has demonstrated the ability to lower blood glucose levels in genetically diabetic mice, indicating its potential role in diabetes research. Additionally, glycyrin exhibits antibacterial properties, making it applicable in studies related to infectious diseases.

Cat. No.

A40013

CAS No.

286390-03-2

9-HEPE

9-HEPE is a PPAR ligand derived from the oxidation of Eicosapentaenoic acid, comprising a racemic mixture of 9(R)-HEPE and 9(S)-HEPE. It enhances fatty acid oxidation, promotes adipogenesis, and increases glucose uptake through the activation of peroxisome proliferator-activated receptors (PPARs) in vivo. This compound is instrumental for research applications focusing on metabolic regulation and disorders related to obesity and insulin sensitivity.

Cat. No.

A40018

CAS No.

1060968-92-4

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.

Cat. No.

A40028

CAS No.

242473-63-8

SKLB102

SKLB102 is a potent PPARγ ligand that demonstrates high affinity for the nuclear receptor. It effectively reduces fat deposition and offers protective effects against non-alcoholic fatty liver disease (NAFLD) by modulating adipocytokine expression and preventing insulin resistance. This compound is valuable for research focused on metabolic disorders and the regulation of lipid metabolism.

Cat. No.

A40052

CAS No.

23953-39-1

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.

Cat. No.

A40063

CAS No.

52936-64-8

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.

Cat. No.

A40064

CAS No.

95520-87-9

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.

Cat. No.

A40069

CAS No.

18446-70-3

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.

Cat. No.

A40076

CAS No.

2089159-00-0

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.

Cat. No.

A40079

CAS No.

1067214-81-6

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.