PPAR Agonist

Rac-Pemafibrate-¹³C,d₃ (Rac-K13675-¹³C,d₃) is the deuterium and ¹³C-labeled Rac-Pemafibrate (HY-17618A). Pemafibrate racemate (K13675 racemate) is the racemate of pemafibrate, and activates PPARα activity, with EC₅₀s of 1 nM, >10 μM and 1.7 μM for h-PPARα, h-PPARγ and h-PPARδ, respectively.

K-111 (BM-170744) is an oral active PPAR alpha agonist. K-111 show efficacy in improving insulin resistance, reducing body weight, and ameliorating atherogenic dyslipidemia. K-111 can be used for study of type 2 diabetes, dyslipidaemia, obesity and the metabolic syndrome.

PPARγ agonist 17 (Compound C1) is a PPARγ agonist. PPARγ agonist 17 enhances PPARγ activity and blocks the cell cycle in G2/M phase, inhibits cell migration and induces apoptosis in HT-29 cells. PPARγ agonist 17 has a broad spectrum anti-proliferative activity in cancer cells with relatively low toxicity in normal cells which cannot cross the blood-brain barrier.

PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC₅₀: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%).

PPARγ agonist 7 (Compound 3a) is a potent and selective agonist of PPARγ. PPARγ agonist 7 promotes adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs) as a novel PPARγ full agonist (EC₅₀, 4.34 μM).

Oxeglitazar is an orally active compound that can be used for the research of type II diabetes.

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.

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.

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].

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.

(+)-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.