PPAR Agonist

Seladelpar (Standard) is the analytical standard of Seladelpar. This product is intended for research and analytical applications. Seladelpar (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM. Seladelpar shows more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively. Seladelpar can be used for the study of primary biliary cholangitis.

4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity, used for cancer and inflammation research.

Fenofibric acid-¹³C₈ (FNF acid-¹³C₈) is ¹³C labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC₅₀s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC₅₀ of 48 nM.

5-Aminosalicylic acid-d₃ disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

Troglitazone (Standard) is the analytical standard of Troglitazone. This product is intended for research and analytical applications. Troglitazone is an orally active PPARγ agonist, with EC₅₀s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.

GW 590735 (Standard) is the analytical standard of GW 590735 (HY-106278). This product is intended for research and analytical applications. GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC₅₀=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia.

N-Desmethyl rosiglitazone (SB 237216) is a metabolite of Rosiglitazone (HY-17386), generated through demethylation by the cytochrome P450 enzyme system in liver microsomes. It retains partial PPARγ agonist activity and supports studies on the metabolism and pharmacokinetics of Rosiglitazone (HY-17386).

BMS-687453 (Standard) is the analytical standard of BMS-687453 (HY-10678). This product is intended for research and analytical applications. BMS-687453 is a potent and selective PPARα agonist, with an EC₅₀ and IC₅₀ of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.

FK614 (Standard) is the analytical standard of FK614 (HY-101292). This product is intended for research and analytical applications. FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes.

L-165041 (Standard) is the analytical standard of L-165041. This product is intended for research and analytical applications. L-165041 is a cell permeable PPARδ agonist, with Kis of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively, and induces adipocyte differentiation in NIH-PPARδ cells.

PPARα/γ agonist 5 is a dual PPARα/γ agonist with significant biological activity exhibited at low concentrations. The EC₅₀ of PPARα/γ agonist 5 are 0.358μM and 1.21μM respectively, showing its potential in inhibiting type 2 diabetes and lipid metabolism disorders. PPARα/γ agonist 5 was selected for clinical development due to its high efficacy.

(E/Z)-Elafibranor ((E/Z)-GFT505) is a PPARα/δ agonist with EC₅₀s of 45 and 175 nM, respectively.

Cefminox (sodium) (MT-141) (Standard) is the analytical standard of Cefminox (sodium). This product is intended for research and analytical applications. Cefminox sodium is a semisynthetic cephamycin, which exhibits antibacterial activity. Cefminox sodium is a broad-spectrum, bactericidal cephalosporin antibiotic. Cefminox sodium also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ. Cefminox sodium upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium also prevents pulmonary arterial hypertension in rat model.

Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC₅₀ of 0.8 nM for growth inhibition.

Farglitazar (Standard) is the analytical standard of Farglitazar (HY-105074). This product is intended for research and analytical applications. Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients.

Bezafibrate-¹³C₆ (BM15075-¹³C₆) is ¹³C labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC₅₀s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.

17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid (17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA) is an electrophilic oxo-derivative (EFOX) of the docosahexaenoic acid (DHA) (HY-B2167). 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is generated during inflammation by COX-2-catalyzed mechanism in activated macrophages. 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid acts as an agonist for PPARγ and a modulator for NF-κB signaling pathway, inhibits the production of pro-inflammatory cytokines and nitric oxide, and exhibits anti-inflammatory efficacy.

5-Aminosalicylic acid-d₇ (5-ASA-d₇; Mesalamie-d₇; Mesalazie-d₇) is deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

Elafibranor (Standard) is the analytical standard of Elafibranor. This product is intended for research and analytical applications. Elafibranor (GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively. Elafibranor can be used for the study of primary biliary cholangitis.

SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model.