PPAR

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.

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.

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.

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.

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.

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.

Cat. No.

A40085

CAS No.

1168138-37-1

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.

Cat. No.

A40096

CAS No.

227002-04-2

L-764406

L-764406 is a high-affinity non-thiazolidinedione ligand for the peroxisome proliferator-activated receptor gamma (PPARγ). Demonstrating partial agonist activity, L-764406 activates the expression of adipocyte-specific genes, such as aP2, in both chimeric receptors containing the PPARγ ligand-binding domain and in 3T3-L1 cell models. Notably, L-764406 does not exhibit activity with PPARα or PPARδ, making it a selective tool for studying PPARγ-related pathways and their implications in metabolic research.

Cat. No.

A40127

CAS No.

685139-10-0

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.

Cat. No.

A40134

CAS No.

3024531-27-6

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.

Cat. No.

A40142

CAS No.

321557-86-2

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.

Cat. No.

A40143

CAS No.

3322-62-1

(E/Z)-Oleamide

Synonyms: Octadec-9-enamide

(E/Z)-Oleamide is a potent ligand for the peroxisome proliferator-activated receptor alpha (PPARα). This compound, derived from the plant Galium aparine L., plays a crucial role in modulating hippocampal plasticity through the transcriptional activation of cyclic AMP response element-binding protein (CREB). Its biological activities include the regulation of feeding and sexual behavior in rodent models, making it significant for research in neurobiology and metabolism.

Cat. No.

A40173

CAS No.

1030594-28-5

(+)-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.