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  1. NF-κB Immunology/Inflammation Apoptosis
  2. Keap1-Nrf2 STING Apoptosis
  3. Omaveloxolone

Omaveloxolone  (Synonyms: RTA 408)

目錄號(hào): HY-12212 純度: 99.40%
COA 產(chǎn)品使用指南

Omaveloxolone (RTA 408) 是一種抗氧化炎癥調(diào)節(jié)劑 (AIM),可激活 Nrf2 并抑制一氧化氮 (NO)。Omaveloxolone 通過(guò)抑制 STING 依賴(lài)的 NF-κb 信號(hào)通路,來(lái)抑制破骨細(xì)胞的生成。

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Omaveloxolone Chemical Structure

Omaveloxolone Chemical Structure

CAS No. : 1474034-05-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥1342
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2 mg ¥990
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5 mg ¥1100
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10 mg ¥1700
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25 mg ¥3060
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50 mg ¥4900
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Customer Review

    Omaveloxolone purchased from MCE. Usage Cited in: Redox Biol. 2020 Jan;28:101309.  [Abstract]

    The protein level of STING was analyzed by western blotting on day 2 and 4 of osteoclastogenesis in the presence of RTA-408.

    Omaveloxolone purchased from MCE. Usage Cited in: Redox Biol. 2020 Jan;28:101309.  [Abstract]

    F-Actin ring formation assays are carried to detect the effect of RTA-408 on the generation of mature osteoclasts. The actin rings were detected using phalloidin with fluorescence microscopy after RTA-408 treatment (20 nM).

    Omaveloxolone purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:7612182.  [Abstract]

    Nuclear translocation of Nrf2 by RTA-408 is measured by immunohistochemistry staining.
    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.

    IC50 & Target

    Nrf2[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HT-29 EC50
    1.41 μM
    Compound: 12; RTA-408
    Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
    Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
    [PMID: 33248849]
    L929 EC50
    5.25 μM
    Compound: 12; RTA-408
    Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
    Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
    [PMID: 33248849]
    體外研究
    (In Vitro)

    為評(píng)估 Omaveloxolone (RTA 408) 的抗炎活性,用 Omaveloxolone 處理 RAW 264.7 小鼠巨噬細(xì)胞兩個(gè)小時(shí),然后添加 IFNγ 以刺激 NO 產(chǎn)生并釋放到培養(yǎng)基中。Omaveloxolone 以劑量依賴(lài)性方式降低培養(yǎng)基中的 NO 濃度,IC50 值為 4.4±1.8 nM。Omaveloxolone 在此測(cè)定中的效力與 Bardoxolone methyl 的效力相似,后者的 IC50 值為 1.9±0.8 nM。AIM 介導(dǎo)的 NO 抑制需要 Nrf2 激活。在 bardoxolone 甲基處理的 RAW 264.7 細(xì)胞中觀(guān)察到一氧化氮合酶 2 (Nos2) 蛋白水平降低,當(dāng) siRNA 降低 Nrf2 mRNA 水平時(shí),該蛋白水平減弱。為評(píng)估 Omaveloxolone 的抗癌活性,一組來(lái)自不同來(lái)源腫瘤的八種人類(lèi)細(xì)胞系用 Omaveloxolone 處理,并在 72 小時(shí)后使用磺酰羅丹明 B (SRB) 測(cè)定法測(cè)量細(xì)胞生長(zhǎng)。Omaveloxolone 抑制所有腫瘤細(xì)胞系的生長(zhǎng),平均 GI50 值為 260±74 nM。為確定 Omaveloxolone 是否誘導(dǎo)細(xì)胞凋亡,用 Omaveloxolone 和半胱天冬酶底物 DEVD-AFC 處理一組腫瘤細(xì)胞 24 小時(shí)。Omaveloxolone 以劑量依賴(lài)性方式增加 DEVD-AFC 裂解,表明 Omaveloxolone 處理會(huì)觸發(fā)癌細(xì)胞中的 caspase 激活。在增加 DEVD-AFC 裂解的相同濃度的 Omaveloxolone 下,蛋白質(zhì)印跡也觀(guān)察到 Caspase-3 和 caspase-9 裂解[1]

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

    體內(nèi)研究
    (In Vivo)

    為確定 Omaveloxolone (RTA-408) 是否是骨髓致死劑量的全身照射 (TBI) 后造血急性放射綜合征的有效緩解劑,小鼠在 TBI 后 24 小時(shí)開(kāi)始每天注射 3 次 17.5 mg/kg Omaveloxolone。Omaveloxolone 處理導(dǎo)致 100% 的 7 Gy (LD40/35) TBI 小鼠 (P<0.05) 和 60% 的 7.5 Gy (LD100/13) TBI 小鼠 (P<0.0001)[2]。

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

    Clinical Trial
    分子量

    554.71

    Formula

    C33H44F2N2O3

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 100 mg/mL (180.27 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(kāi)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 1.8027 mL 9.0137 mL 18.0274 mL
    5 mM 0.3605 mL 1.8027 mL 3.6055 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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.51 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      1 mL 工作液為例,取 100 μL 25.0 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

    由于實(shí)驗(yàn)過(guò)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(guò) 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)。
    您所需的儲(chǔ)備液濃度超過(guò)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(guò)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

    純度: 99.52%

    參考文獻(xiàn)
    Cell Assay
    [1]

    MEFs, PANC-1, A549, A375, A549/NF-κB-Luc and HeLa/NF-κB-Luc cells are cultured in Gibco high glucose DMEM with 10% FBS. G-361 cells are cultured in McCoy’s 5A medium with 10% FBS. All other cell lines are cultured in RPMI 1640 medium with 10% FBS. For growth inhibition assays, cells are plated in duplicate 96-well culture dishes at 3×103 cells per well. The following day, one plate is treated with Omaveloxolone (200, 400, 600, 800 and 1000 nM) and the other is immediately processed for the sulforhodamine B (SRB) assay (time 0). Cells in the Omaveloxolone-treated plate are processed for the SRB assay 72 hours after the start of treatment. Percentage of growth relative to vehicle-treated cells is calculated. Dose-response curves are plotted in GraphPad Prism and GI50 values are calculated. For cell counting experiments, MEFs are plated in 6-well culture dishes at 5×104 cells per well and treated with Omaveloxolone the following day. Following treatment, cells are counted using a Vi-CELL XR cell analyzer. For clonogenic assays, wild-type (1×103 cells per well) and Keap1-/- (0.5×103 cells per well) MEFs are seeded in 6-well dishes. Six hours later, MEFs are treated with Omaveloxolone. After seven days, colonies are fixed with a 1:7 solution of acetic acid:MeOH and stained with 0.5% crystal violet in MeOH. Colonies consisting of ≥50 cells are counted[1].

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

    Animal Administration
    [2]

    Mice[2]
    For radiation survival experiments, wild-type C57Bl/6 CD45.2 mice (6-8 weeks old) are used. Congenic wild-type C57Bl/6 CD45.1 and C57Bl/6 CD45.1/CD45.2 hybrid host mice are used as recipients in transplantation experiments. Omaveloxolone stock solutions for vehicle control (DMSO) are prepared within 1 h before injection. Omaveloxolone (17.5 mg/kg) or DMSO is administered intraperitoneally at 24, 48 and 72 h after irradiation. Whole-body irradiation (7-8 Gy) is performed using a 250-kVp X-ray machine with 50 cm source-to-skin distance and a 2 mm copper filter. The dose rate is approximately 1.4 Gy/min.

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

    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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(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 1.8027 mL 9.0137 mL 18.0274 mL 45.0686 mL
    5 mM 0.3605 mL 1.8027 mL 3.6055 mL 9.0137 mL
    10 mM 0.1803 mL 0.9014 mL 1.8027 mL 4.5069 mL
    15 mM 0.1202 mL 0.6009 mL 1.2018 mL 3.0046 mL
    20 mM 0.0901 mL 0.4507 mL 0.9014 mL 2.2534 mL
    25 mM 0.0721 mL 0.3605 mL 0.7211 mL 1.8027 mL
    30 mM 0.0601 mL 0.3005 mL 0.6009 mL 1.5023 mL
    40 mM 0.0451 mL 0.2253 mL 0.4507 mL 1.1267 mL
    50 mM 0.0361 mL 0.1803 mL 0.3605 mL 0.9014 mL
    60 mM 0.0300 mL 0.1502 mL 0.3005 mL 0.7511 mL
    80 mM 0.0225 mL 0.1127 mL 0.2253 mL 0.5634 mL
    100 mM 0.0180 mL 0.0901 mL 0.1803 mL 0.4507 mL
    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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    產(chǎn)品名稱(chēng):
    Omaveloxolone
    目錄號(hào):
    HY-12212
    需求量: