PPARα Agonist

XYQ3-B11 is a potent PPARα agonist with an EC₅₀ of 8.33 μM. XYQ3-B11 activates PPARα. XYQ3-B11 can be used for the research of dyslipidemia.

Cevoglitazar (LBM-642) is an orally active and highly potent PPARα and PPARγ dual agonist. Cevoglitazar can reduce food intake, body weight, and fasting plasma insulin in obese mice and cynomolgus monkeys. Cevoglitazar has the potential for diabetes and obesity-related disorders research.

HSD17B13/PPAR modulator-1 (Compound 17) is a HSD17B13/PPAR multitarget modulator. HSD17B13/PPAR modulator-1 is an inhibitor of HSD17B13, with its IC₅₀ value being 0.91 μM. HSD17B13/PPAR modulator-1 is a PPAR agonist, with the EC₅₀ values for PPARα, PPARδ, and PPARγ being 1.55, 0.12, and 0.01 μM respectively. HSD17B13/PPAR modulator-1 can significantly improve liver function, regulate lipid metabolism, alleviate fibrosis, and exert antioxidant and anti-inflammatory effects in the model of metabolic dysfunction-related steatohepatitis (MASH). HSD17B13/PPAR modulator-1 can be used for the study of MASH.

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.

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.

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.

DN203316 (PPARδ agonist 11) is a potent, selective, orally active PPARδ agonist (EC₅₀ = 20 nM) with high selectivity over PPARα and PPARγ. DN203316 suppresses NF-κB-mediated inflammatory signaling, inhibits ferroptosis by upregulating xCT and GPX4, and attenuates STING-TBK1-IRF3-driven fibrogenic responses. DN203316 is useful for research on inflammatory disorders, metabolic dysfunction-associated steatohepatitis (MASH), and liver fibrosis.

PPARα/δ agonist 3 (Compound 8) is the orally active agonist for PPAR, that activates PPARα, PPARδ and PPARγ with EC₅₀s of 5.6, 3.4 and 1278 nM, respectively. PPARα/δ agonist 3 exhibits anticholestatic activity in mouse ANIT- or CDCA (HY-76847)-induced cholestatic liver disease models.

PPARα agonist 1 is a potent and full hPPARα agonist.

Ciprofibrate (Standard) is the analytical standard of Ciprofibrate. This product is intended for research and analytical applications. Ciprofibrate (Win35833) is a potent peroxisome proliferator and increases the phosphorylation level of the PPARalpha. Ciprofibrate acts as an orally active hypolipidaemic agent and can be used for the research of primary hyperlipidaemias.

PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC₅₀ values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent.

PPARδ agonist 13 is a potent, selective and orally active PPARδ agonist with an EC₅₀ values of 0.50 nM. PPARδ agonist 13 binds to the PPARδ ligand-binding pocket and upregulates PPARδ target gene expression. PPARδ agonist 13 inhibits renal fibroblast activation, restores fatty acid oxidation, and attenuates TGF-β1-induced renal fibroblast activation. PPARδ agonist 13 exhibits anti-renal fibrosis effects in a mouse model of unilateral ureteral obstruction. PPARδ agonist 13 can be used for the research of renal fibrosis.

PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC₅₀ values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes.

Elaidyl-sulfamide (N-(9E)-9-Octadecen-1-ylsulfamide) is a PPARα agonist. Elaidyl-sulfamide reduces body weight gain and food intake and reduces circulating cholesterol levels and increases both glucose and insulin levels. Elaidyl-sulfamide has the potential for the research of complicated obesity.

Sitofibrate is a Clofibrate (HY-B0287) derivative. Sitofibrate is aperoxisome proliferator activated receptor-α (PPAR-α) agonist. Sitofibrate is an antihyperlipidemic agent.

GW 2433 is a dual PPARα and PPARδ agonist. GW 2433 has the potential for the study of type II diabetes and dyslipidemia.

ZINC17167211 is a potent PPAR-α agonist (EC₅₀=0.16 nM) that can be used in the study of diabetes, hyperlipidemia, and inflammatory diseases.

TZD18 is a potent and orally active PPARα and PPARγ dual agonist with IC₅₀ values of 0.028, 0.057, >10 µM for PPARα, PPARγ, PPARδ, respectively. TZD18 reduces plasma levels of both glucose and triglycerides in diabetic mice. TZD18 has the potential for the research of type 2 diabetes.

AVE-8134 is a potent PPARα agonist, with EC₅₀ values of 100 and 3000 nM for human and rodent PPARα receptor, respectively.