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  3. Rosiglitazone potassium

Rosiglitazone potassium  (Synonyms: BRL 49653 potassium)

目录号: HY-17386B
产品使用指南

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。

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Rosiglitazone potassium Chemical Structure

Rosiglitazone potassium Chemical Structure

CAS No. : 316371-84-3

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Rosiglitazone potassium 的其他形式现货产品:

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MCE 顾客使用本产品发表的 98 篇科研文献

WB
IF
Cell Viability Assay

    Rosiglitazone potassium purchased from MCE. Usage Cited in: Carcinogenesis. 2023 Mar 31;bgad015.  [Abstract]

    Rosiglitazone (ROSI; 15, 30, 60, 120, 240 µM; 24 h) significantly inhibits the growth of NCI-H929 and OPM-2 cells.

    Rosiglitazone potassium purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.  [Abstract]

    Protein levels of BACE1 and APP are measured by western blot assay in cerebral cortex of 12-month-old AD mice with different treatments (RSG and GW9662).

    Rosiglitazone potassium purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.  [Abstract]

    Protein levels of sAPPα and sAPPβ are measured by western blot assay in cerebral cortex of 12-month-old AD mice with different treatments (RSG and GW9662).

    Rosiglitazone potassium purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.  [Abstract]

    PPARγ level is determined by IF assay in 3×Tg-AD mice, 3×Tg-AD mice with RSG treatment, 3×Tg-AD-KO mice, 3×Tg-AD-KO mice with GW9662 stimulation.

    Rosiglitazone potassium purchased from MCE. Usage Cited in: Free Radic Biol Med. 2018 Aug 21;126:259-268.  [Abstract]

    Laser confocal microscope is performed to measure MMP indicated with the ratio of JC-1 Red/JC-1 Green. Nuclei are counterstained with DAPI (blue). Bar graphs represent the mean ± SD of red/green fluorescence intensity.

    Rosiglitazone potassium purchased from MCE. Usage Cited in: Front Mol Neurosci. 2017 Sep 14;10:293.  [Abstract]

    Rosiglitazone enhances the phosphorylation of insulin receptor substrate 1 (IRS1, phosphorylated at Ser 636/639), which is considered to be the main activator of the Akt/mTOR pathway by IGF-1R.

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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].

    IC50 & Target[1][2][4]

    PPARγ

    40 nM (Kd)

    PPARγ

    60 nM (EC50)

    TRPC5

    30 μM (EC50)

    TRPM3

     

    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 IC50 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 (HY-10162)‑induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells[7].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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.
    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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.
    Clinical Trial
    分子量

    395.52

    Formula

    C18H18KN3O3S

    CAS 号
    中文名称

    罗格列酮钾盐

    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.

    纯度 & 产品资料
    参考文献
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Rosiglitazone potassium
    目录号:
    HY-17386B
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