PPAR Agonist

BR101549 is a non-TZD agonist of PPARγ. BR101549 activates PPARγ to the level of Pioglitazone in vitro. BR101549 can control blood glucose level in mouse model. BR101549 can be studied in anti-diabetic research.

PPARγ agonist 16 (Compound 4G) is the agonist for PPARγ, that competitively binds to LBD domain of PPARγ with IC₅₀ of 1790 nM. PPARγ agonist 16 inhibits the ear swelling in mouse model, and exhibits anti-hyperglycemic in Streptozotocin (HY-13753)-induced mouse diabetes mellitus model.

L-165461 is a PPARδ and PPARγ agonist with K_i values of 3 nM and 15 nM, respectively. L-165461 can be used for research on diabetes.

KD-3010 is a potent, orally active, and selective PPARδ agonist.

PPARα/δ agonist 4 is a potent orally active and selective dual peroxisome proliferator-activated receptor (PPAR) α/δ agonist with EC₅₀s of 0.36 and 1.31 nM, respectively. PPARα/δ agonist 4 exhibits >123-fold selectivity over PPARγ (EC₅₀ = 160.84 nM). PPARα/δ agonist 4 upregulates expression of downstream fatty acid oxidation genes PDK4, CPT1A, and ACADVL. PPARα/δ agonist 4 can be used for the research of metabolic dysfunction-associated steatohepatitis.

PPARγ agonist 8 is an agonist of PPARγ. PPARγ agonist 8 induces peroxisome proliferator response element (PPRE)-luciferase activity with an EC₅₀ of 0.2 μM.

Clofibrate-d₄ is the deuterium labeled Clofibrate. Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.

Flurbiprofen axetil solution is mainly composed of Flurbiprofen axetil (HY-101481). Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway.

DS-6930 is a potent and selective agonist of PPARγ, with an EC₅₀ of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes.

Romazarit (RO 31-3948) is an anti-inflammatory agent with antirheumatic effect. Romazarit exhibits PPARα agonist activity. Romazarit (30 mg/kg) inhibits the development of hindpaw inflammation in an adjuvant arthritis model.

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.

15-Deoxy-Δ12,14-Prostaglandin J2-2-glyceryl ester is a derivate of 15-Deoxy-Δ-12,14-prostaglandin J2 (HY-108568). 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC₅₀ of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC₅₀ of 7 μM.

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.

PPARα agonist 5 is an orally available, selective partial agonist of PPARα (EC₅₀: 3 nM). PPARα agonist 5 reduces lipid accumulation and upregulates key PPARα target genes, exerting anti-fatty liver effects. PPARα agonist 5 also exhibits significant hypolipidemic and hypoglycemic effects through partial PPARγ agonist activity and mild inhibition of protein tyrosine phosphatase 1B (PTP1B) (IC₅₀: 79.1 μM). PPARα agonist 5 has a good safety profile and can be used in the study of type 2 diabetes with dyslipidemia.

KRP-105 is a potent, highly selective, and orally effective PPAR alpha (EC₅₀ = 8 nM) agonist. KRP-105 can significantly reduce serum triglyceride, total cholesterol, and non high density lipoprotein cholesterol levels. KRP-105 can be used for research on metabolic diseases such as dyslipidemia.

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.

LTD4 antagonist 3 (FK011 hydrochloride) is a LTD₄ antagonist. LTD4 antagonist 3 has agonistic activity for PPAR-γ, with a fold-increase of 1.50 at 1 μM and 2.35 at 10 μM. LTD4 antagonist 3 can be used of development of non-steroidal anti-inflammatory drugs (NSAIDs).

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