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.

A16309

CAS No.

1361504-77-9

DG172 dihydrochloride

DG-172 is an orally active potent PPARβ/δ inverse agonist (IC50 = 26.9 nM). DG-172 inhibits Angptl4 gene expression in mouse myoblasts (IC50 = 9.5 nM) in vitro.

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.

A39909

CAS No.

2924573-90-8

FX-909

FX-909 is a covalent inverse agonist of peroxisome proliferator-activated receptor gamma (PPARG), functioning through modulation of receptor activity. This compound exhibits promising biological activity by inhibiting PPARG-mediated signaling pathways, which are often implicated in cancer progression. FX-909 is utilized in cancer research to investigate the effects of PPARG inhibition on tumor growth and survival, providing insights into potential therapeutic targets.

Cat. No.

A39938

CAS No.

423150-91-8

BAY-4931

BAY-4931 is a selective inverse agonist of PPARγ, exhibiting potent action with an IC50 of 0.17 nM. This compound effectively modulates PPARγ activity, making it a valuable tool for investigating metabolic disorders and insulin sensitivity. Its unique mechanism of action allows for detailed studies of PPARγ's role in various biological processes and therapeutic applications.

Cat. No.

A39939

CAS No.

1356497-91-0

ST247

ST247 is a potent inverse agonist of the peroxisome proliferator-activated receptor beta/delta (PPARβ/δ). It exhibits a high affinity for this target and modulates the expression of the activation marker CCL2 in a manner contrary to typical agonist activity. ST247 effectively promotes the interaction with corepressors and inhibits agonist-induced transcriptional activity of PPARβ/δ. This compound is valuable for research into metabolic disorders and inflammation, offering insights into the regulatory mechanisms mediated by PPARβ/δ.

Cat. No.

A39960

CAS No.

2891706-79-7

BAY-5516

BAY-5516 is an inverse agonist of PPARG, exhibiting an IC50 value of 6.1 ± 3.6 nM. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research into cancer therapeutics. It is suitable for studies focusing on the modulation of PPARG signaling pathways and their implications in various tumor models.

Cat. No.

A39978

CAS No.

1415321-64-0

SR10221

SR10221 is a noncovalent inverse agonist of peroxisome proliferator-activated receptor gamma (PPARγ). This compound exhibits significant biological activity by repressing downstream PPARγ target genes, which contributes to growth inhibition in bladder cancer cell lines. SR10221 is primarily utilized in research applications aimed at understanding PPARγ signaling pathways and developing potential therapeutic strategies for bladder cancer.

Cat. No.

A39989

CAS No.

420826-65-9

BAY-0069

BAY-0069 is a selective inverse agonist of PPARγ, exhibiting potent inhibition with IC50 values of 6.3 nM for human PPARγ and 24 nM for mouse PPARγ. This compound serves as a valuable tool for investigating the roles of PPARγ in cancer research, providing insights into its regulatory mechanisms in tumorigenesis and potential therapeutic strategies. Its high selectivity enhances its utility in experimental settings.

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.

A40010

CAS No.

2891706-78-6

BAY-5094

BAY-5094 is an inverse agonist of the peroxisome proliferator-activated receptor gamma (PPARG). This compound exhibits oral bioactivity and has potential applications in the study of luminal bladder cancer. Its mode of action allows for investigation into the role of PPARG in tumorigenesis and cancer progression.

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.

A40092

CAS No.

2891706-83-3

BAY-9683

BAY-9683 is an orally active covalent inverse agonist of PPARG (Peroxisome Proliferator-Activated Receptor Gamma). It effectively inhibits the activity of overactive PPARG, making it a valuable tool for investigating diseases associated with PPARG dysregulation, including luminal bladder cancer. This compound is suitable for research applications focused on metabolic regulation and cancer biology.

Cat. No.

A40122

CAS No.

1415252-61-7

SR2595

SR2595 is an inverse agonist of peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting an IC50 value of 30 nM. This compound functions by modulating PPARγ activity, leading to alterations in gene expression associated with lipid metabolism and insulin sensitivity. SR2595 is primarily used in research related to metabolic disorders, obesity, and diabetes, making it a valuable tool for studying PPARγ signaling pathways and their implications in various physiological processes.

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.

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.