PPAR Agonist

5-Aminosalicylic Acid-d₃ (hydrochloride) is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

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.

Desmethyl Sibutramine (hydrochloride) (Standard) is the analytical standard of Desmethyl Sibutramine (hydrochloride). This product is intended for research and analytical applications. Icosabutate is an orally active engineered fatty acid and a dual FFAR1/FFAR4 (GPR40/GPR120) agonist with EC₅₀ values of 10 μM and 15.5 μM, respectively. Icosabutate acts as a partial agonist of PPAR-α, with an EC₅₀ of 208 nM. Icosabutate inhibits the arachidonic acid cascade and exhibits antioxidant and anti-apoptotic activities. Icosabutate can be used in the research of nonalcoholic steatohepatitis, metabolic dysfunction-associated steatohepatitis, and atherosclerosis.

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.

PPARγ agonist-26 is a PPARγ agonist with an EC₅₀ of 98.43 μM. PPARγ agonist-26 is non-cytotoxic and does not inhibit α-glucosidase. PPARγ agonist-26 induces migration of HEK 293 cells. PPARγ agonist-26 can be used for research on PPAR-γ-related diseases, such as diabetes.

11-cis-Retinoic Acid-d₅ is the deuterium labeled Retinoic acid. 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[1][2].

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.

WAY-120744 is a novel naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxide.

Fenofibrate-13C6 is a deuterated labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.

Magnolol (Standard) is the analytical standard of Magnolol. This product is intended for research and analytical applications. Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 μM and 17.7 μM, respectively.

Rosiglitazone (hydrochloride) (Standard) is the analytical standard of Rosiglitazone (hydrochloride). This product is intended for research and analytical applications. Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer.

Balaglitazone (Standard) is the analytical standard of Balaglitazone. This product is intended for research and analytical applications. Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.

GW7647 (Standard) is the analytical standard of GW7647. This product is intended for research and analytical applications. GW7647 is a potent PPARα agonist, with EC50s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.

Inolitazone (dihydrochloride) (Standard) is the analytical standard of Inolitazone (dihydrochloride). This product is intended for research and analytical applications. Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.

Sipoglitazar is an orally active agonist of PPAR. Sipoglitazar can be used to study diabetes.

Flurbiprofen axetil (Standard) is the analytical standard of Flurbiprofen axetil. This product is intended for research and analytical applications. 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.

Pirinixic acid (Standard) is the analytical standard of Pirinixic acid. This product is intended for research and analytical applications. Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.

Prostaglandin B₃ (PGB₃) is a member of the class of prostaglandins B and a secondary alcohol. PGB₃ exhibits a rather low affinity to human PPARγ with a K_i value greater than 1 mM compared with K_i values of 26.28 ± 8.7 μM for PGB₁ and 77 ± 37.7 μM for PGB₂.

(+)-Arhalofenate ((+)-MBX 102) is the less active enantiomer of Arhalofenate (HY-14831). Arhalofenate is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.

RG-12525 (Standard) is the analytical standard of RG-12525 (HY-101676). This product is intended for research and analytical applications. RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 μM.