Rosiglitazone

Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer^[1][2][4][7]. IC50 & Target: EC50: 30 nM (PPARγ1), 100 nM (PPARγ2)^[1], 60 nM (PPARγ)^[2], appr 30 nM (TRPC5)^[4]
Kd: appr 40 nM (PPARγ)^[1]
IC50: appr 22.5 μM (TRPM2)^[4] In Vitro: Rosiglitazone (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes^[1].
Rosiglitazone (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons^[3].
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^[3].
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^[4].
Rosiglitazone (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation^[7].
Rosiglitazone (5 μM, 7 days) suppresses Olaparib (HY-10162)‑induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells^[7]. In Vivo: Rosiglitazone (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats^[5].
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^[6].
Rosiglitazone (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models^[7].