CYP3 Modulator

PIPE-791 is an orally active, blood-brain barrier-permeable selective antagonist of LPAR1. PIPE-791 inhibits LPA-induced calcium mobilization, collagen expression, histamine release, and the activation of fibroblasts, microglia and macrophages. PIPE-791 induces oligodendrocyte precursor cell differentiation, myelination and remyelination, and increases the number of microglia in the retina of normotensive rats. PIPE-791 protects mature oligodendrocytes from cytokine-induced death, reduces the levels of pulmonary fibrosis markers and alleviates neuroinflammation in preclinical models. PIPE-791 can be used in the research of glaucoma, neuroinflammatory diseases, chronic osteoarthritis pain, idiopathic pulmonary fibrosis and multiple sclerosis.

N-Desmethyl-Apalutamide, the major active metabolite of Apalutamide (HY-16060), is a selective competitive inhibitor of androgen receptor. N-Desmethyl-Apalutamide is catalyzed by CYP3A4 and CYP2C8 enzymes. The plasma protein binding rate of N-Desmethyl-Apalutamide reaches 95%, with albumin as the primary binding protein. N-Desmethyl-Apalutamide is suitable for prostate cancer-related research.