Rosiglitazone (BRL 49653) 是一种具有口服活性的PPARγ选择性激动剂 (EC50: 60 nM,Kd: 40 nM)。Rosiglitazone 是一种TRPC5激活剂 (EC50: 30 μM) 和TRPM3抑制剂。Rosiglitazone 可用于肥胖、糖尿病、衰老、卵巢癌的研究。
| 生物活性 | Rosiglitazone (BRL 49653) is an orally active selectivePPARγagonist (EC50: 60 nM,Kd: 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, 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 (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 IC50values 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].
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 (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].
| 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 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(699.44 mM;Need ultrasonic) Ethanol : 2 mg/mL(5.60 mM;ultrasonic and warming and heat to 60℃) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) 配制储备液 | 1 mM | 2.7978 mL | 13.9888 mL | 27.9775 mL | | 5 mM | 0.5596 mL | 2.7978 mL | 5.5955 mL | | 10 mM | 0.2798 mL | 1.3989 mL | 2.7978 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: 2.5 mg/mL (6.99 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.99 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 2. 请依序添加每种溶剂： 5% DMSO 40%PEG300 5%Tween-80 50% saline Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution 3. 请依序添加每种溶剂： 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution 4. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.82 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 5. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.82 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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