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  2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel Autophagy Apoptosis
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  4. Rosiglitazone hydrochloride

Rosiglitazone hydrochloride  (Synonyms: 鹽酸羅格列酮; BRL 49653 hydrochloride)

目錄號(hào): HY-17386A 純度: 99.31%
COA 產(chǎn)品使用指南 技術(shù)支持

Rosiglitazone (BRL 49653) hydrochloride 是一種具有口服活性的 PPARγ 選擇性激動(dòng)劑 (EC50: 60 nM, Kd: 40 nM)。Rosiglitazone hydrochloride 是一種 TRPC5 激活劑 (EC50: 30 μM) 和 TRPM3 抑制劑。Rosiglitazone hydrochloride 可用于肥胖、糖尿病、衰老、卵巢癌的研究。

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Rosiglitazone hydrochloride Chemical Structure

Rosiglitazone hydrochloride Chemical Structure

CAS No. : 302543-62-0

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥660
In-stock
50 mg ￥600
In-stock
100 mg ￥1050
In-stock
200 mg ￥1800
In-stock
500 mg   詢價(jià)  
1 g   詢價(jià)  

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Customer Review

Other Forms of Rosiglitazone hydrochloride:

MCE 顧客使用本產(chǎn)品發(fā)表的 104 篇科研文獻(xiàn)

WB
IF
Cell Viability Assay

    Rosiglitazone hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride 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

     

    體外研究
    (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 IC50 values 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].

    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: 1 μM
    Result: Increased NF-α1 and BCL-2 protein level.
    體內(nèi)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].

    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

    393.89

    Formula

    C18H20ClN3O3S
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    鹽酸羅格列酮
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式

    -20°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 62.5 mg/mL (158.67 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.5388 mL 12.6939 mL 25.3878 mL
    5 mM 0.5078 mL 2.5388 mL 5.0776 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 10 mg/mL (25.39 mM); 澄清溶液

      此方案可獲得 ≥ 10 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 100.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: 10 mg/mL (25.39 mM); 懸濁液; 超聲助溶

      此方案可獲得 10 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 100.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5388 mL 12.6939 mL 25.3878 mL 63.4695 mL
    5 mM 0.5078 mL 2.5388 mL 5.0776 mL 12.6939 mL
    10 mM 0.2539 mL 1.2694 mL 2.5388 mL 6.3469 mL
    15 mM 0.1693 mL 0.8463 mL 1.6925 mL 4.2313 mL
    20 mM 0.1269 mL 0.6347 mL 1.2694 mL 3.1735 mL
    25 mM 0.1016 mL 0.5078 mL 1.0155 mL 2.5388 mL
    30 mM 0.0846 mL 0.4231 mL 0.8463 mL 2.1156 mL
    40 mM 0.0635 mL 0.3173 mL 0.6347 mL 1.5867 mL
    50 mM 0.0508 mL 0.2539 mL 0.5078 mL 1.2694 mL
    60 mM 0.0423 mL 0.2116 mL 0.4231 mL 1.0578 mL
    80 mM 0.0317 mL 0.1587 mL 0.3173 mL 0.7934 mL
    100 mM 0.0254 mL 0.1269 mL 0.2539 mL 0.6347 mL
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    產(chǎn)品名稱：
    Rosiglitazone hydrochloride
    目錄號(hào)：
    HY-17386A
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