Rosiglitazone

A potent and selective PPARγ agonist that binds to the PPARγ ligand-binding domain with a Kd of 40 nM; an antidiabetic agent that has been used as an oral hypoglycemic agent in the treatment of Type II diabetes; also inhibits TRP channels TRPM2 and TRPM3 with IC50 of 22.5 uM and 5-10 uM, respectively; also increases klotho and decreases Wnt5A in tumor cells.Diabetes Approved (In Vitro) :Rosiglitazone (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes.Rosiglitazone (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons.Rosiglitazone (1 μM, 24 h) protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner.Rosiglitazone (0.01-100 μM, 15 min) inhibits TRPM3 with IC50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively.Rosiglitazone (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation.Rosiglitazone (5 μM, 7 days) suppresses Olaparib (HY-10162) induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells. (In Vivo) :Rosiglitazone (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats.Rosiglitazone (intraperitoneal injection, 3 mg/kg/day) ameliorates airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα in male Wistar rats.Rosiglitazone (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models.