Rosiglitazone (BRL 49653) hydrochloride 是一种具有口服活性的PPARγ选择性激动剂 (EC50: 60 nM,Kd: 40 nM)。Rosiglitazone hydrochloride 是一种TRPC5激活剂 (EC50: 30 μM) 和TRPM3抑制剂。Rosiglitazone hydrochloride 可用于肥胖、糖尿病、衰老、卵巢癌的研究。
| 生物活性 | Rosiglitazone (BRL 49653) hydrochloride is an orally active selectivePPARγagonist (EC50: 60 nM,Kd: 40 nM). Rosiglitazone hydrochloride is aTRPC5activator (EC50: 30 μM) andTRPM3inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovariancancer[1][2][4][7]. |
| IC50& Target[1][2][4] | PPARγ 40 nM (Kd) | PPARγ 60 nM (EC50) | TRPC5 30 μM (EC50) | TRPM3 |
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体外研究
(In Vitro) | Rosiglitazone hydrochloride (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes[1].
Rosiglitazone hydrochloride (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons[3].
Rosiglitazone hydrochloride (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 hydrochloride (0.01-100 μM, 15 min) inhibits TRPM3 with IC50values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively[4].
Rosiglitazone hydrochloride (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation[7].
Rosiglitazone hydrochloride (5 μM, 7 days) suppresses Olaparib (HY-10162)-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: | 1 μM | | Result: | Increased NF-α1 and BCL-2 protein level. |
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体内研究
(In Vivo) | Rosiglitazone hydrochloride (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats[5].
Rosiglitazone hydrochloride (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 hydrochloride (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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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