MKEY, a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, has been shown to protect against atherosclerosis and aortic aneurysm formation by mediating inflammation, but whether it modulates neuroinflammation and brain injury has not
Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy.
Forodesine hydrochloride (BCX-1777 hydrochloride), a potent inhibitor of human lymphocyte proliferation, effectively induces apoptosis in leukemic cells by elevating dGTP levels. This compound is an orally active, highly potent purine nucleoside phosphorylase (PNP) inhibitor, demonstrating IC50 values between 0.48 to 1.57 nM across human, mouse, rat, monkey, and dog PNP.