Rosiglitazone (BRL 49653) potassium 是一种具有口服活性的PPARγ选择性激动剂 (EC50: 60 nM,Kd: 40 nM)。Rosiglitazone potassium 是一种TRPC5激活剂 (EC50: 30 μM) 和TRPM3抑制剂。Rosiglitazone potassium 可用于肥胖、糖尿病、衰老、卵巢癌的研究。

Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist ( EC 50 : 60 nM, K d : 40 nM). Rosiglitazone potassium is a TRPC5 activator ( EC 50 : 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer [1] [2] [4] [7].

Rosiglitazone potassium (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes [1]. Rosiglitazone potassium (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons [3]. Rosiglitazone potassium (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 potassium (0.01-100 μM, 15 min) inhibits TRPM3 with IC 50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively [4]. Rosiglitazone potassium (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation [7]. Rosiglitazone potassium (5 μM, 7 days) suppresses Olaparib induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells [7]. Cell Proliferation Assay [7] Cell Line: A2780 and SKOV3 cells Concentration: 0.5-50 μM Incubation Time: 1-7 days Result: Inhibited cell proliferation in a time dependent and concentration dependent manner. Western Blot Analysis [3] Cell Line: Hippocampal neurons Concentration: 1 μM Incubation Time: 24 h Result: Increased NF-α1 and BCL-2 protein level.

Rosiglitazone potassium (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats [5]. Rosiglitazone potassium (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 potassium (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models [7]. Animal Model: Streptozotocin (STZ)-induced diabetic rats [5] Dosage: 5 mg/kg Administration: Oral administration, daily for 8 weeks. Result: Decreased IL-6, TNF-α, and VCAM-1 levels in diabetic group. Displayed lower levels of lipid peroxidation and NOx with an increase in aortic GSH and SOD levels compared to diabetic groups. Animal Model: Male Wistar rats [6] Dosage: 3 mg/kg/day Administration: Intraperitoneal injection, twice a day, 6 days per week for 12 consecutive weeks Result: Ameliorated emphysema, elevated PEF, and higher level of total cells, neutrophils and cytokines (TNF-α and IL-1β) induced by cigarette smoke (CS). Inhibited CS-induced M1 macrophage polarization and decreased the ratio of M1/M2.

316371-84-3

C18H18KN3O3S

395.52

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years