PPAR Agonist

OLHHA is a dual CB1 receptor antagonist and PPARα agonist. OLHHA also is a alcohol intake inhibitor with an EC₅₀ value of 0.2 mg/kg. OLHHA reduces both hepatic lipid accumulation and circulating triglyceride levels. OLHHA shows anti-steatotic activity and has the potential for the research of non-alcoholic fatty liver disease (NAFLD).

Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate (Win35833) is a potent peroxisome proliferator, increases the phosphorylation level of the PPARalpha.

PPARα/γ agonist 3 (Compound 4) is a dual agonist of PPARα/γ. PPARα/γ agonist 3 has anti-inflammatory activity, significantly reducing inflammatory markers such as IL-6 and MCP-1 on THP-1 macrophages through NF-κB activation. PPARα/γ agonist 3 can be used in the study of metabolic syndrome and metabolic dysfunction-related fatty liver disease (MAFLD).

BMS711939 is a selective agonist for peroxisome proliferator-activated receptor α (PPAR α), with EC₅₀ of 4 nM and 4.5 μM, for human PPARα and human PPARγ. BMS711939 exhibits good pharmacokinetic characters in rats models. BMS711939 increases HDL cholesterol, reduces LDL cholesterol and triglycerides.

MBX-102 acid is a selective partial PPAR-γ agonist. MBX-102 acid binds highly to plasma proteins, mainly serum albumin. MBX-102 acid can be used to study type 2 diabetes.

Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC₅₀ value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity..

Isobutylparaben (Standard) is the analytical standard of Isobutylparaben. This product is intended for research and analytical applications. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics.

MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC₅₀ being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC₅₀ values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ.

PPARγ agonist-23 (Compound 9) is an orally active PPARγ agonist with an EC₅₀ of 0.32 μM. PPARγ agonist-23 improves hepatic triglyceride levels, reduces scores of steatosis and hepatocellular ballooning, and decreases the total activity score of non-alcoholic steatohepatitis (NASH). PPARγ agonist-23 can be used for the research of non-alcoholic steatohepatitis.

ZLY032 is a dual FFA1/PPARδ agonist with the activity of improving glucose and lipid metabolism, alleviating liver fibrosis, and potentially inhibiting metabolic disorders.

Pparδ agonist 7 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 7 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2019105234A1, compound TM4).

Pparδ agonist 8 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 8 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2021169769A1, compound TM2).

5-cis Carbaprostacyclin is a stable analog of PGI2 based on Carbaprostacyclin (HY-112322). Carbacyclin is a PGI2 receptor agonist and vasodilator that activates PPARδ. 5-cis Carbaprostacyclin induces relaxation of pulmonary vascular tone.

EL244 is a dua Autotaxin (ATX) (IC₅₀ = 50 nM) inhibitor and PPARγ (IC₅₀ = 1.3 μM; K_d = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC₅₀ = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research.

PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC₅₀s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy.

Isosilybin A (Standard) is the analytical standard of Isosilybin A (HY-N7043). Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity^[1][2][3].

E-3030 free acid is a potent dual activator of peroxisome proliferator-activated receptor (PPAR) alpha and PPARgamma, exhibiting significant antidiabetic and lipid-modulating effects. E-3030 decreases blood glucose, triglyceride, non-esterified fatty acids, and insulin levels, while increasing blood adiponectin levels. E-3030 improves glucose tolerance and shows remarkable triglyceride- and non-high-density lipoprotein cholesterol-lowering effects in animal models.

L-796449 is a potent PPARγ agonist. L-796449 shows neuroprotective. L-796449 has the potential for the research of stroke.

LJ570 is a PPARα/PPARγ dual agonist with EC₅₀s of 1.05 and 0.12 μM, respectively.

Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC₅₀ of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation.