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  2. Metabolic Enzyme/Protease Anti-infection
  3. Phosphodiesterase (PDE) RSV
  4. Roflumilast

Roflumilast  (Synonyms: 羅氟司特; APTA-2217; BYK 20869; B9302-107)

目錄號(hào): HY-15455 純度: 99.98%
COA 產(chǎn)品使用指南

Roflumilast (APTA-2217) 是一種選擇性的 PDE4 抑制劑，作用于 PDE4A1，PDEA4，PDEB1 和 PDEB2，IC50 分別為 0.7，0.9，0.7 和 0.2 nM。

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Roflumilast Chemical Structure

Roflumilast Chemical Structure

CAS No. : 162401-32-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥605
In-stock
5 mg ￥498
In-stock
10 mg ￥649
In-stock
25 mg ￥1460
In-stock
50 mg ￥2481
In-stock
100 mg ￥3474
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Roflumilast:

    Roflumilast purchased from MCE. Usage Cited in: Int Urol Nephrol. 2019 Feb;51(2):253-260.  [Abstract]

    Increased protein expression levels of inflammatory factors are deceased after oral Roflumilast treatment in diabetic rat DSM.

    Roflumilast purchased from MCE. Usage Cited in: Int Urol Nephrol. 2017 Oct;49(10):1723-1730.  [Abstract]

    Oral Roflumilast treatment attenuates increased expression of inflammatory factor protein in obese rat bladder. Comparison of protein expression levels of NF-κB, IL-6 in the DSM. The data are the ratio of target protein with reference. The protein levels of vehicle-treated HFDfed rats are significantly higher than those of the ND+vehicle group. The protein levels of Roflumilast-treated HFD-fed rats are significantly reduced compared to vehicle-treated HFD-fed rats. Data are shown as relative pro

    查看 Phosphodiesterase (PDE) 亞型特異性產(chǎn)品:

    • 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

    Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.

    IC50 & Target

    PDE4

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK293 IC50
    1 nM
    Compound: Roflumilast
    Inhibition of PDE4 expressed in HEK293 cells coexpressing cyclic nucleotide gated ion channel mutant assessed as inhibition of NECA-induced cAMP production treated 15 mins before NECA challenge measured after 45 mins by FLIPR assay
    Inhibition of PDE4 expressed in HEK293 cells coexpressing cyclic nucleotide gated ion channel mutant assessed as inhibition of NECA-induced cAMP production treated 15 mins before NECA challenge measured after 45 mins by FLIPR assay
    		[PMID: 20378348]
    PBMC IC50
    0.02 nM
    Compound: Roflumilast
    Inhibition of TNFalpha production in LPS-stimulated human PBMC preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay
    Inhibition of TNFalpha production in LPS-stimulated human PBMC preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay
    		[PMID: 19256507]
    PBMC EC50
    50 nM
    Compound: Roflumilast
    Anti-inflammatory activity against human PBMCs assessed as reduction in LPS-induced TNF-alpha release by ELISA analysis
    Anti-inflammatory activity against human PBMCs assessed as reduction in LPS-induced TNF-alpha release by ELISA analysis
    		[PMID: 33569941]
    Sf9 IC50
    5.8 nM
    Compound: CHEMBL193240
    Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate
    Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate
    		[PMID: 26908025]
    Splenocyte IC50
    1.2 nM
    Compound: Roflumilast
    Inhibition of LPS-induced TNFalpha production in Balb/c mouse splenocytes after 18 to 24 hrs by AlphaLISA assay
    Inhibition of LPS-induced TNFalpha production in Balb/c mouse splenocytes after 18 to 24 hrs by AlphaLISA assay
    		[PMID: 24094436]
    Splenocyte IC50
    1.2 nM
    Compound: 1
    Antiinflammatory activity in Balb/c mouse splenocytes assessed as LPS-induced TNF-alpha production after 18 to 24 hrs by AlphaLISA
    Antiinflammatory activity in Balb/c mouse splenocytes assessed as LPS-induced TNF-alpha production after 18 to 24 hrs by AlphaLISA
    		[PMID: 23602400]
    體外研究
    (In Vitro)

    Roflumilast 不影響除 PDE4 之外的 PDE 酶，并且是大多數(shù)測試的 PDE4 剪接變體的亞納摩爾抑制劑。除了 PDE4C (4C1，IC50=3 nM；4C2，IC50=4.3 nM) 外，它沒有表現(xiàn)出 PDE4 亞型選擇性，它被抑制的效力略低[2]。Roflumilast 是一種有效的選擇性 PDE4 抑制劑。Roflumilast 是一種單選擇性 PDE4 抑制劑，因?yàn)樗挥绊懫渌?PDE 同工酶，包括濃度高達(dá) 10，000 倍的 PDE1、PDE2、PDE3 和 PDE5。Roflumilast 抑制人中性粒細(xì)胞功能。Roflumilast 抑制單核細(xì)胞來源的樹突狀細(xì)胞中的 TNFα 合成。Rolfumilast 抑制 CD4+ T 細(xì)胞的增殖和細(xì)胞因子合成。效力 (IC30) 為 7 nM 的 Roflumilast 最多可抑制增殖約 60%[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Roflumilast 的動(dòng)物研究表明，在豚鼠、小鼠或大鼠短期暴露于煙草煙霧以及大鼠暴露于煙草煙霧和細(xì)菌脂多糖的組合后，它減少了支氣管肺泡灌洗液中嗜中性粒細(xì)胞的積累，并消除了暴露于煙草煙霧 7 個(gè)月的大鼠肺實(shí)質(zhì)炎癥細(xì)胞流入[2]。Roflumilast 在 pIgR / 小鼠中阻斷 COPD 進(jìn)展。對于這些研究，9 個(gè)月大的 WT 或 pIgR / 小鼠每天通過口服強(qiáng)飼法處理 100 μg Roflumilast (5 μg/g) 或載體 (4% 甲基纖維素，1.3% PEG400) 3 個(gè)月，肺在 12 個(gè)月大時(shí)收獲。與載體處理的 pIgR-/- 小鼠不同，Roflumilast 處理的小鼠在開始處理后小氣道壁重塑沒有進(jìn)展。引人注目的是，與 9 個(gè)月大的 pIgR / 小鼠相比，Roflumilast 處理的 12 個(gè)月大的 pIgR / 小鼠肺氣腫指數(shù)降低，表明 Roflumilast 不僅阻止了該模型中肺氣腫的進(jìn)展，而且顯然有助于解決肺實(shí)質(zhì)的肺氣腫性破壞[4]。

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

    403.21

    Formula

    C17H14Cl2F2N2O3
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    羅氟司特
    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 : ≥ 50 mg/mL (124.00 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.4801 mL 12.4005 mL 24.8010 mL
    5 mM 0.4960 mL 2.4801 mL 4.9602 mL
    查看完整儲(chǔ)備液配制表

    * 請根據(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?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?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

      請依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.20 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。

      以 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。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    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)備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(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，請謹(jǐn)慎選擇該方案。
    請確保第一步儲(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: 99.98%

    參考文獻(xiàn)
    Kinase Assay
    [3]

    PDE activity is determined with some modifications. The assay mixture contain 50 mM Tris (pH 7.4), 5 mM MgCl2, 0.5 μM cAMP or cGMP, and [3H]cAMP or [3H]cGMP (about 30,000 cpm/assay), the indicated concentration of the inhibitor and an aliquot of the enzyme solution at a final assay volume of 200 μL. Stock solutions of the compounds are diluted 1:100 (v/v) in the Tris buffer mentioned above; appropriate dilutions are prepared in 1% (v/v) DMSO/Tris buffer, which are diluted 1:2 (v/v) in the assays to obtain the desired final concentrations of the inhibitors at a DMSO concentration of 0.5% (v/v). DMSO itself affected none of the PDE activities. After preincubation for 5 min at 37°C, the reaction is started by the addition of substrate (cAMP or cGMP) and the assays are incubated for further 15 min at 37°C. Then 50 μL of 0.2 N HCl is added to stop the reaction and the assays are left on ice for about 10 min. Following incubation with 25 μg of 5′-nucleotidase (Crotalus atrox snake venom) for 10 min at 37°C, the assays are loaded on QAE Sephadex A-25 (1 mL of bed volume in Poly-Prep chromatography columns). The columns are eluted with 2 mL of 30 mM ammonium formate (pH 6.0) and the eluate is counted for radioactivity. Results are corrected for blank values (measured in the presence of denatured protein) that are below 5% of total radioactivity. The amount of cyclic nucleotides hydrolyzed did not exceed 30% of the original substrate concentration[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Mice[4]
    WT or pIgR?/? mice are used. For studies using Roflumilast, 200 μL of 0.5 mg/mL suspension of Roflumilast or vehicle (4% methylcellulose, 1.3% PEG400 and 5 μg drug per g animal weight) is administered by oral gavage once daily, 5 days a week for the duration of treatment. Mice are treated daily by oral gavage with 100 μg of Roflumilast (5 μg/g) or vehicle (4% methylcellulose, 1.3% PEG400) for 3 months and lungs are harvested at 12 months of age.

    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?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?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 2.4801 mL 12.4005 mL 24.8010 mL 62.0024 mL
    5 mM 0.4960 mL 2.4801 mL 4.9602 mL 12.4005 mL
    10 mM 0.2480 mL 1.2400 mL 2.4801 mL 6.2002 mL
    15 mM 0.1653 mL 0.8267 mL 1.6534 mL 4.1335 mL
    20 mM 0.1240 mL 0.6200 mL 1.2400 mL 3.1001 mL
    25 mM 0.0992 mL 0.4960 mL 0.9920 mL 2.4801 mL
    30 mM 0.0827 mL 0.4133 mL 0.8267 mL 2.0667 mL
    40 mM 0.0620 mL 0.3100 mL 0.6200 mL 1.5501 mL
    50 mM 0.0496 mL 0.2480 mL 0.4960 mL 1.2400 mL
    60 mM 0.0413 mL 0.2067 mL 0.4133 mL 1.0334 mL
    80 mM 0.0310 mL 0.1550 mL 0.3100 mL 0.7750 mL
    100 mM 0.0248 mL 0.1240 mL 0.2480 mL 0.6200 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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    Inquiry Information

    產(chǎn)品名稱：
    Roflumilast
    目錄號(hào)：
    HY-15455
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