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.

A15651

CAS No.

36052-37-6

Alpinetin

Alpinetin is a flavonoid that acts as a PPAR-γ activator, demonstrating significant anti-inflammatory and hepatoprotective properties. It effectively inhibits lipopolysaccharide (LPS)-induced inflammation and protects against LPS-induced renal injury by modulating TLR4 expression and activating the Nrf2 pathway. Its diverse biological activities make Alpinetin a valuable reagent for research into tumor biology, cardiovascular health, and neuroprotection.

Cat. No.

A15680

CAS No.

521-32-4

Bilobetin

Bilobetin acts as a PPARα activator, enhancing lipid metabolism and insulin sensitivity. It effectively reduces blood lipid levels by promoting hepatic lipid uptake and oxidation, while decreasing triglyceride secretion and accumulation in tissues. Additionally, Bilobetin stimulates the phosphorylation and nuclear translocation of PPARα, resulting in increased cAMP levels and PKA activity. This compound is significant for research in metabolic disorders, particularly those related to insulin resistance and lipid regulation.

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.

A15707

CAS No.

66056-22-2

Angeloylgomisin H

Angeloylgomisin H is a PPAR-γ activator derived from the lignin extract of Schisandra rubriflora. This compound has demonstrated the ability to enhance insulin-stimulated glucose uptake, making it a valuable candidate for research in metabolic disorders and diabetes. Its mechanism of action may provide insights into therapeutic strategies aimed at improving insulin sensitivity and glucose metabolism.

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.

A21411

CAS No.

331744-72-0

Peliglitazar racemate

Synonyms: BMS 426707-01 racemate; BMS-426707-01

Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator.

Cat. No.

A26090

CAS No.

774603-05-3

12-Nitrolinoleate

Synonyms: 12-Nitro-9-cis,12-cis-octadecadienoic acid

12-Nitrolinoleate is a potent peroxisome proliferator-activated receptor γ (PPARγ) activator derived from linoleic acid through nitration. It effectively induces PPARγ-dependent gene expression in MCF-7 cells, demonstrating an EC50 of 0.045 μM. Additionally, 12-Nitrolinoleate exhibits anti-inflammatory properties by inhibiting NF-κB transcription in RAW 264.7 cells, along with reducing levels of pro-inflammatory cytokines such as IL-6, TNF-α, and CCL2 in response to LPS stimulation. This compound is valuable for research applications focused on metabolic regulation and inflammation.

Cat. No.

A39730

CAS No.

316371-83-2

Rosiglitazone sodium

Synonyms: BRL 49653 sodium

Rosiglitazone sodium is a potent and selective activator of the peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting EC50 values of 30 nM, 100 nM, and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, with a Kd of approximately 40 nM. In addition to its role as a PPARγ activator, Rosiglitazone sodium functions as a modulator of transient receptor potential (TRP) channels, specifically inhibiting TRP melastatin 2 (TRPM2) and TRPM3, while activating TRP canonical 5 (TRPC5). This compound is utilized in research related to metabolic disorders, obesity, and other conditions linked to PPARγ signaling.

Cat. No.

A39915

CAS No.

508-75-8

Convallatoxin

Convallatoxin is a PPARγ activator derived from the plant Adonis amurensis. It exhibits significant anti-inflammatory effects by mitigating colitic inflammation through the activation of PPARγ and the suppression of NF-κB signaling pathways. Additionally, Convallatoxin serves as a substrate for P-glycoprotein, identifying Val982 as a critical amino acid for its transport. This compound also enhances ligand-induced micro-opioid receptor (MOR) endocytosis, demonstrating high potency and efficacy, making it valuable for research in inflammation and cellular signaling.

Cat. No.

A39916

CAS No.

60008-02-8

Glabrone

Glabrone, a PPAR-γ activator derived from the roots of Glycyrrhiza glabra, demonstrates notable ligand binding activity to this nuclear receptor. In addition to its role as a specific probe substrate for UGT1A9, Glabrone's metabolites inhibit neuraminidase, thus preventing influenza virus release. This compound is suitable for research applications focused on herb-drug interactions and the evaluation of anti-influenza viral activity.

Cat. No.

A39918

CAS No.

29623-28-7

(S)-Coriolic acid

Synonyms: 13(S)-HODE

(S)-Coriolic acid is a potent PPARγ activator formed through the metabolism of linoleic acid by 15-lipoxygenase (15-LOX). This compound serves as a crucial intracellular signaling agent, influencing cell proliferation and differentiation across diverse biological systems. Additionally, (S)-Coriolic acid is known to induce mitochondrial dysfunction and contribute to airway epithelial injury, making it relevant for studies investigating cellular stress responses and respiratory health.

Cat. No.

A39920

CAS No.

59403-52-0

SDPC

Synonyms: PC(18:0/22:6); DHA-PC; 1-Stearoyl-2-docosahexaenoyl-sn-glyerco-3-phosphocholine

SDPC (DHA-PC) is a PPARγ activator that demonstrates significant anti-angiogenic properties. This phospholipid, featuring an ester bond with docosahexaenoic acid (DHA) at the sn-2 position, effectively inhibits the proliferation, migration, and tube formation of human umbilical vein endothelial cells. SDPC holds potential for applications in anti-tumor angiogenesis research, making it a valuable tool for studying tumor progression and vascular growth inhibition.

Cat. No.

A39935

CAS No.

2420-56-6

(10E,12Z)-Octadeca-10,12-dienoic acid

Synonyms: trans-10,cis-12 CLA2

(10E,12Z)-Octadeca-10,12-dienoic acid is a potent PPARα activator that plays a critical role in regulating lipid metabolism and adipocyte differentiation. This compound has demonstrated various biological activities, including antioxidant and antitumor effects, alongside the induction of proinflammatory cytokines and chemokines, which may contribute to decreased adipogenesis and insulin resistance. (10E,12Z)-Octadeca-10,12-dienoic acid also influences milk fat synthesis by reducing the expression of lipogenic enzymes and inhibiting fatty acid desaturation. Additionally, it has been shown to modulate lipoprotein lipase activity in cultured adipocytes and alter hepatic stearoyl-CoA desaturase expression in vivo.

Cat. No.

A39955

CAS No.

2921-20-2

2-(Tetradecylthio)acetic acid

2-(Tetradecylthio)acetic acid is a pan-peroxisome proliferator-activated receptor (pan-PPAR) activator. This compound is known to induce hypolipidemia by reducing plasma lipid levels and enhancing hepatic fatty acid oxidation in rodent models. Additionally, it increases the expression of genes associated with fatty acid uptake, activation, accumulation, and oxidation, making it a valuable tool for research on lipid metabolism and related disorders.

Cat. No.

A39964

CAS No.

98462-03-4

8(S)-HETE

Synonyms: 8(S)-Hydroxyeicosatetraenoic acid

8(S)-HETE (8(S)-Hydroxyeicosatetraenoic acid) primarily acts as a PPARα activator, with demonstrated biological activity in stimulating mouse keratinocyte protein kinase C at an IC50 of 100 μM. This compound selectively activates PPARα at concentrations as low as 0.3 μM, making it valuable for research into skin biology and inflammatory responses. The stereochemical assignment of the (S) enantiomer is confirmed through chiral HPLC retention time comparisons with established data.

Cat. No.

A39987

CAS No.

3086376-13-5

SP4f

SP4f is a potent PPAR-γ activator, exhibiting an EC50 of 826 nM in HK-2 cells. This compound has been shown to lower blood glucose levels and decrease lipid peroxidation, while also enhancing glutathione levels and catalase activity in Swiss albino mice. SP4f is valuable for research focused on metabolic regulation, diabetes, and oxidative stress.

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.

A40014

CAS No.

79551-84-1

20-Carboxyarachidonic acid

20-Carboxyarachidonic acid is an endogenous dual activator of PPARalpha and PPARgamma. As a stable metabolite of 20-HETE, it plays a significant role in regulating lipid metabolism and inflammation. This compound is utilized in research exploring metabolic disorders, cardiovascular diseases, and the modulation of inflammatory responses.

Cat. No.

A40017

CAS No.

3086376-12-4

SP4e

SP4e is a selective activator of peroxisome proliferator-activated receptor gamma (PPAR-γ), exhibiting an EC50 of 739 nM in HK-2 cells. This compound displays significant biological activity by lowering blood glucose levels and reducing lipid peroxidation, while simultaneously enhancing glutathione levels and catalase activity in Swiss albino mice. SP4e can be employed in research focused on metabolic disorders, oxidative stress, and related therapeutic pathways.

Cat. No.

A40025

CAS No.

29623-29-8

13-Oxo-9E,11E-octadecadienoic acid

13-Oxo-9E,11E-octadecadienoic acid acts as a potent PPARα activator and is derived from tomato juice. This compound has demonstrated the ability to reduce plasma and hepatic triglyceride levels in obese diabetic mouse models. Its applications in research include the study of metabolic disorders and potential therapeutic strategies for obesity-related conditions.

Cat. No.

A40027

CAS No.

2909474-29-7

E0924G

E0924G is an orally active PPARδ activator with an EC50 of 2.82 μM. This compound effectively induces the upregulation of osteoprotegerin (OPG) with an EC50 of 0.29 μM, demonstrating significant inhibition of RANKL-induced osteoclast differentiation and F-actin ring formation in RAW264.7 macrophages. E0924G has potential applications in research focused on bone density regulation and the treatment of bone loss in models of ovariectomized and age-related osteoporosis.

Cat. No.

A40051

CAS No.

331744-64-0

Peliglitazar

Synonyms: BMS 426707-01

Peliglitazar is a dual alpha and gamma peroxisome proliferator-activated receptor (PPAR) activator. It promotes insulin sensitivity and lipid metabolism, making it valuable in the study of metabolic disorders such as type 2 diabetes and obesity. Research applications include investigating the molecular mechanisms of PPAR signaling and developing therapeutic strategies for related conditions.

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.