PPAR Agonist

Reglitazar is an agonist for peroxisome proliferator-activated receptor α and β (PPAR α and PPAR β), which enhances insulin sensitivity, lowers blood glucose and regulates blood lipid levels.

MHY 553 is a PPARα agonist that is effective when taken orally. MHY 553 helps alleviate liver fat accumulation by increasing fatty acid oxidation and reducing inflammation during the aging process. MHY 553 inhibits the accumulation of triglycerides induced by liver X receptor agonists in HepG2 cells. MHY 553 significantly suppresses the expression of inflammatory mRNA in aging rats.

Retinoic acid-d₃ is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC₅₀s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.

BM 170249 is a peroxisome proliferator, particularly in the perivenous region of the central acini in the liver. BM 170249 significantly reduces serum triglyceride and cholesterol levels in rats. BM 170249 strongly induces the activity of key enzymes in the peroxisome fatty acid β-oxidation system (such as acyl-CoA oxidase AOX, multifunctional enzyme PH, and thiolase PT), but leads to decreased activity of catalase and uricase in peroxisome components. BM 170249 could be used in lipid-lowering studies.

dual FXR/PPARδ agonist-2 is a FXR/PPARδ dual agonist through hybridation of FXR agonist GW-4064 and PPARδ agonist GW-0742.dual FXR/PPARδ agonist-2 displays potent dual-target activities with a FXR agonistic EC₅₀ of 12.28 nM and 69 % PPARδ activation at 100 nM. dual FXR/PPARδ agonist-2 shows anti-fibrotic effects in pulmonary fibrosis mouse model.

Rosiglitazone-d₄-1 (BRL 49653-d₄-1) is deuterium-labeled Rosiglitazone (HY-17386).

MHY908 is a potent dual agonist of PPARα and PPARγ. MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity.

Dehydroabietic acid (Standard) is the analytical standard of Dehydroabietic acid. This product is intended for research and analytical applications. Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice.

17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid (17-Oxo-DHA) is a metabolite of lipoxygenase-mediated oxidation of DHA. 17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid is a PPARγ agonist and activates a Nrf2 dependent antioxidant reaction.

PPARα agonist 3 (Compound A229) is a PPARα agonist (EC₅₀: 590 nM). PPARα agonist 3 inhibits TBHP or 4-HNE (HY-113466)-induced production of ROS.

LS2265 is a taurine derivative of fenofibrate and can induce proliferation of peroxisomes in liver cells of rats.

KRP-297 is a PPARα and PPARγ agonist potentially for the research of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver.

CS4 is a selective HDAC inhibitor with the IC₅₀ values of 38 nM, 12 nM, 5.8 μM, 19 μM and 61 μM against of HDAC1, HDAC6, HDAC8, HDAC4 and HDAC11, respectively. CS4 promotes α-tubulin and histone 3 acetylation. CS4 activates PPARγ and blocks glycolysis. CS4 induces cell cycle arrest at G2 phase and apoptosis, and shows anticancer effect both in vivo and in vitro.

PPARγ agonist 12 (compound 9i) is a potent and selective PPARγ agonist with EC₅₀s of 3.98 and 15.42 μM against PPARγ and PPARδ, respectively. PPARγ agonist 12 improves insulin secretion and has anti-diabetic effect.

KRP-101 is a compound that regulates the expression of genes related to lipid metabolism. It is a PPARα agonist that can highly sensitively regulate the expression of genes such as apolipoprotein A-IV, which may be related to lowering serum triglycerides and increasing HDL.

PPAR agonist 6 (compound 5a) is an agonist of PPAR with EC₅₀ values of 3.6 μM, 2.6 μM, and 2.7 μM for PPARα, PPARβ/δ, and PPARγ, respectively. PPAR agonist 6 represses the transactivation of the TNFα-dependent NF-κB-driven reporter in L929 cells.

GW0072 is a partial agonist of PPARγ and does not directly bind to the AF-2 helix of PPARγ, resulting in specific partial receptor transcriptional activation properties.

LY-510929 is a compound that induces left ventricular hypertrophy (LVH). Related studies have identified the relevant conditions in which LY-510929 may induce LVH by measuring multiple markers and using multiple techniques.

VSP-77 is an orally active PPARγ agonist. VSP-77 selectively upregulates the expression of insulin sensitivity-related genes (Glut4 and Adiponectin) by inhibiting CDK5-mediated phosphorylation of PPARγ at Ser-273. VSP-77 significantly improves glucose tolerance, reduces fasting blood glucose and insulin levels in high-fat diet (HFD)-induced diabetic mouse models. VSP-77 can be used for the study of diabetes.

Rac-Pemafibrate-¹³C,d₃ (Rac-K13675-¹³C,d₃) is the deuterium and ¹³C-labeled Rac-Pemafibrate (HY-17618A). Pemafibrate racemate (K13675 racemate) is the racemate of pemafibrate, and activates PPARα activity, with EC₅₀s of 1 nM, >10 μM and 1.7 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively.