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.

A13346

CAS No.

118414-82-7

MK 886

Synonyms: L-663,536; L663536

MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).

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.

A15044

CAS No.

856676-23-8

Choline Fenofibrate

Synonyms: ABT-335

Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia.

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.

A17602

CAS No.

75498-96-3

Cefminox Sodium (MT-141)

Synonyms: MT-141

Cefminox Sodium, also known as Meicelin and MT-141, is a penicillin binding protein inhibitor used to treat bacterial infection.

Cat. No.

A19368

CAS No.

1133819-87-0

Azemiglitazone {MSDC-0602)

Synonyms: MSDC 0602

MSDC-0602, a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and are effective for treatment of type 2 diabetes with reducing risk of PPARγ-mediated side effects.

Cat. No.

A20815

CAS No.

251303-04-5

Ertiprotafib

Synonyms: PTP 112

Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.

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.

A24175

CAS No.

2791417-66-6

MTX-531

MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia.

Cat. No.

A24326

CAS No.

495-02-3

Auraptene

Auraptene is an orally active geranyloxycoumarin compound naturally found in plants of the *Brassicaceae* family. It exhibits a wide range of biological activities, including antibacterial, anti-pathogenic, antioxidant, anti-tumor, and neuroprotective effects. Auraptene has shown therapeutic potential in the management of various chronic conditions such as hypertension and cystic fibrosis, making it a valuable compound for pharmacological and nutraceutical research.

Cat. No.

A29089

CAS No.

1825345-52-5

AZ0108

AZ0108 is a selective inhibitor of poly(ADP-ribose) polymerases (PARPs), including PARP1, PARP2, PARP3, PARP6, TNKS1, and TNKS2. It displays potent inhibitory activity with IC50 values of

Cat. No.

A29120

CAS No.

2923687-90-3

AZD-9574-acid

AZD-9574-acid is a selective PPAR-1 inhibitor that serves as a crucial building block for the development of PROTAC molecules. Its inhibition of PPAR-1 demonstrates significant potential in the regulation of metabolic pathways and inflammatory responses. This compound is essential for researchers exploring targeted protein degradation and its applications in therapeutic development.

Cat. No.

A30771

CAS No.

118194-13-1

Soyasaponin Ab

Soyasaponin Ab is a potent PPARγ inhibitor with oral bioavailability. It effectively suppresses PPARγ transcriptional activity and induces apoptosis at elevated concentrations. This compound exhibits a range of biological activities, including anti-obesity, anti-oxidation, anti-inflammation, and anti-aging effects. Additionally, Soyasaponin Ab has been shown to mitigate memory impairment induced by Scopolamine, making it a valuable reagent for research in metabolic and neuroprotective applications.

Cat. No.

A31416

CAS No.

376-06-7

Perfluorotetradecanoic acid

Synonyms: PFTeDA

Perfluorotetradecanoic acid (PFTeDA) is a potent PPARγ inhibitor, demonstrating a binding affinity to the human PPARγ ligand-binding domain with an IC50 of 22.8 μM and a Kd of 157.8 μM. It has been shown to impair Leydig cell function through the induction of oxidative stress and apoptosis. Additionally, PFTeDA stimulates corticosterone biosynthesis while inhibiting aldosterone production, making it a valuable tool for researching steroidogenesis and related metabolic pathways.

Cat. No.

A39202

CAS No.

2016043-80-2

PIISVYWK

PIISVYWK is a potent PPARγ inhibitor that also acts as an activator of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2). This compound effectively modulates the HO-1/Nrf2 signaling pathway, contributing to the reduction of oxidative stress and inflammation, while also exhibiting anti-obesity properties. PIISVYWK is suitable for research applications focused on obesity and related metabolic disorders.

Cat. No.

A39908

CAS No.

19879-30-2

Bavachinin

Synonyms: 7-O-Methylbavachin; Bavachinin A

Bavachinin is a pan-peroxisome proliferator-activated receptor (PPAR) agonist and a HIF-1α inhibitor, demonstrating IC50 values of 21.043 μM, 12.819 μM, and 0.622 μM for PPAR-α, PPAR-β/δ, and PPAR-γ, respectively. This compound exhibits significant antitumor activity against non-small cell lung cancer through its modulation of PPAR-γ. Additionally, Bavachinin possesses notable anti-inflammatory and anti-angiogenic properties, making it a valuable tool for research in cancer and metabolic disorders. Its oral bioavailability further supports its utility in various biological studies.

Cat. No.

A39919

CAS No.

2682078-97-1

PPARγ-IN-2

PPARγ-IN-2 is a selective PPARγ inhibitor that effectively reduces triglyceride accumulation in 3T3-L1 preadipocytes, with an EC50 of 0.106 μM. This compound demonstrates potential for mitigating obesity and associated metabolic syndrome, particularly in the context of a high-cholesterol diet. Its ability to diminish lipid accumulation in adipose tissue makes it a valuable tool for research focused on metabolic disorders and adipocyte biology.

Cat. No.

A39931

CAS No.

2088135-12-8

SR 16832

SR 16832 is a dual-site covalent inhibitor of peroxisome proliferator-activated receptor gamma (PPARγ). It functions by targeting both orthosteric and allosteric sites, leading to significant modulation of PPARγ activity. This compound is valuable for research applications related to metabolic disorders, obesity, and diabetes, particularly in studies investigating the downstream effects of PPARγ inhibition on gene expression and cellular metabolism.

Cat. No.

A39936

CAS No.

2829349-96-2

FTX-6746

FTX-6746 is an orally active inhibitor of peroxisome proliferator-activated receptor gamma (PPARG). It demonstrates significant tumor inhibition in mouse xenograft models, making it a valuable tool for investigating the therapeutic potential of targeting PPARG in cancer research. Its specificity and efficacy in modulating PPARG activity support its use in studies related to metabolic disorders and cancer biology.

Cat. No.

A39958

CAS No.

4407-36-7

trans-Cinnamyl alcohol

trans-Cinnamyl alcohol is a selective PPARγ inhibitor that plays a significant role in regulating lipid metabolism and adipogenesis. As a metabolite derived from chestnut flowers, it exhibits anti-obesity activity by inhibiting PPARγ expression. This compound is valuable for research applications focused on obesity, metabolic disorders, and the modulation of fat cell differentiation.

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.

A39998

CAS No.

2882975-84-8

PPARγ phosphorylation inhibitor 1

PPARγ phosphorylation inhibitor 1 is a selective inhibitor targeting Peroxisome Proliferator-Activated Receptor gamma (PPARγ). It effectively inhibits CDK5-mediated phosphorylation of PPARγ at Ser273 with an IC50 of 160 nM, demonstrating a binding affinity with an IC50 of 24 nM. This compound exhibits minimal PPARγ agonistic activity in reporter gene assays, making it a valuable tool for studying the role of PPARγ phosphorylation in metabolic disorders and antidiabetic research applications.

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.

A40019

CAS No.

2409685-41-0

Anti-NASH agent 1

Anti-NASH agent 1 is a potent PPAR-α/δ inhibitor that effectively targets nonalcoholic steatohepatitis (NASH). This compound has demonstrated significant efficacy in improving hyperlipidemia, liver fat degeneration, and liver inflammation in a methionine-choline deficiency (MCD) induced NASH mouse model. Additionally, Anti-NASH agent 1 exhibits low liver toxicity while providing protective effects on liver health, making it a valuable tool for research into metabolic disorders and liver diseases.