PPAR Antagonist

MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC₅₀ of 30 nM) and leukotriene biosynthesis (IC₅₀s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.

MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC₅₀ of 30 nM) and leukotriene biosynthesis (IC₅₀s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis.

GW9662-d₅ is the deuterium labeled GW9662. GW9662 is a potent and selective PPARγ antagonist with an IC₅₀ of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.

Leriglitazone-d₄ (MIN-102-d₄; Hydroxypioglitazone-d₄) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penetrable PPARγ agonist with an EC₅₀ of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases.

Anti-osteoporosis agent-10 is an osteoporosis inhibitor. Anti-osteoporosis agent-10 can suppress the generation of osteoclasts, with an IC₅₀ of 0.042 μM. Anti-osteoporosis agent-10 also has antagonistic activity on PPARγ, with an EC₅₀ value of 0.75 μM.

DPP-IV-IN-5 is isolated from the fruits of Lycium barbarum. DPP-IV-IN-5 exerts moderate agonistic activities for peroxisome proliferator-activated receptor (PPARγ) with EC₅₀ values of 10.09 - 44.26 μM and also presents inhibitory activity on dipeptidyl peptidase-4 (DPPIV) with an IC₅₀ value of 47.13 μM .

T0070907 (Standard) is the analytical standard of T0070907. This product is intended for research and analytical applications. T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.

GW6471 (Standard) is the analytical standard of GW6471 (HY-15372). This product is intended for research and analytical applications. GW6471 is a selective peroxisome proliferator-activated receptor α (PPARα) antagonist. GW6471 reduces cancer stem cell viability, proliferation, and spheroid formation. GW6471 induces apoptosis and causes metabolic impairment including energy imbalance. GW6471 can be used for the research of paragangliomas and triple-negative breast cancer.

GSK0660 (Standard) is the analytical standard of GSK0660. This product is intended for research and analytical applications. GSK0660 is a potent PPARβ antagonist with an IC50 of 155 nM.

MK-886 (Standard) is the analytical standard of MK-886. This product is intended for research and analytical applications. MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.

GW9662 (Standard) is the analytical standard of GW9662. This product is intended for research and analytical applications. GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.