PPAR Agonist

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.

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.

GSK-7227 (compound 32) is a PPARδ partial agonist with the activity of regulating the expression of related genes. GSK-7227 has partial agonist effects on PPARδ target genes CPT1a and PDK4 in skeletal muscle cells.

Phellopterin (Standard) is the analytical standard of Phellopterin. Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.

Choline Fenofibrate (Standard) is the analytical standard of Choline Fenofibrate. This product is intended for research and analytical applications. Choline Fenofibrate (ABT-335), a choline salt of Fenofibric acid (HY-B0760), releases free Fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.

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

Pioglitazone ketone is an active metabolite of the PPARγ agonist Pioglitazone (HY-13956). Formation of pioglitazone ketone occurs primarly through cytochrome P450 (CYP) isoform CYP2C8-mediated metabolism of pioglitazone. Pioglitazone ketone (100 mg/kg in the diet) reduces blood glucose levels in a KKAy mouse model of type 2 diabetes.

PPARγ agonist 9 is an agonist of PPARγ. PPARγ agonist 9 is the analogue of lysophosphatidic acid with an EC₅₀ more than 10 μM for LPA₃ receptor.