Metabolism

Lp-PLA2-IN-16 (Example 1) is an inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with potential applications in Alzheimer's disease research [1].

"PPARγ-IN-2 (Compound 5a), a PPARγ inhibitor, exhibits an EC50 of 0.106 μM in inhibiting TG accumulation in 3T3-L1 preadipocytes.

Lp-PLA2-IN-15 (example 2) is an inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with potential application in Alzheimer's disease research [1].

Lp-PLA2-IN-12 (compound 19), an Lp-PLA2 inhibitor, is utilized in researching neurodegenerative diseases including Alzheimer's disease (AD), glaucoma, age-

Mavodelpar free acid (REN001 free acid) is an selective agonist of PPARδ.

IDO1-IN-22 (Compound 3) is an inhibitor of IDO1, demonstrating potent activity with biochemical hIDO1 IC50 of 67.4 nM and HeLa hIDO1 IC50 of 17.6 nM.

URAT1&XO Inhibitor 1 (compound 29) serves as a dual inhibitor with IC50 values of approximately 10 μM for URAT1 and 1.01 μM for Xanthine Oxidase.

SH1573 is an orally active inhibitor of mutant isocitrate dehydrogenase 2 (mIDH2). It selectively targets the mIDH2 R140Q protein with a potent inhibitory effect (IC50=4.78 nmol/L), significantly reducing the production of the oncogenic metabolite 2-hydroxyglutarate (2-HG) in animal models, cell lines, serum, and tumors. SH1573 is utilized in the study of acute myeloid leukemia (AML).

CC15009 is a potent inhibitor of xanthine oxidoreductase (XOR), demonstrating an IC50 value of 0.237 nM. It effectively inhibits the oxidative subtype of XOR, thereby reducing the generation of the byproduct ROS and exhibiting antioxidant activity. CC15009 has shown a favorable dose-dependent uric acid-lowering effect in two different XOR substrate-induced hyperuricemia mouse models.