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。
| 生物活性 |
Rosiglitazone (BRL 49653) potassium is an orally active selectivePPARγagonist (EC50: 60 nM,Kd: 40 nM). Rosiglitazone potassium is aTRPC5activator (EC50: 30 μM) andTRPM3inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovariancancer[1][2][4][7].
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| 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 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 IC50values 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 (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: |
24 h |
| Result: |
Increased NF-α1 and BCL-2 protein level. |
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体内研究
(In Vivo) |
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. |
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| Clinical Trial |
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| 分子量 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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