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  1. Membrane Transporter/Ion Channel Autophagy
  2. CFTR Autophagy
  3. KM11060

KM11060 是 F508 缺失-囊性纖維化跨膜電導(dǎo)調(diào)節(jié)劑 (F508del-CFTR) 轉(zhuǎn)運(yùn)缺陷的校正劑。KM11060 可用于 F508del-CFTR 加工缺陷的研究和囊性纖維化研究劑的開發(fā)。

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KM11060 Chemical Structure

KM11060 Chemical Structure

CAS No. : 774549-97-2

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3.  試用裝只面向終端客戶

規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥390
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5 mg ¥350
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10 mg ¥600
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25 mg ¥1200
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50 mg ¥2200
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100 mg ¥3800
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

WB

    KM11060 purchased from MCE. Usage Cited in: Patent. US9987256B2.

    CFTR correctors (Compounds A to F(KM11060)) promote the rescue of R98H mutant of alpha-sarcoglycan in HEK293 cell model.

    KM11060 purchased from MCE. Usage Cited in: Patent. US20150328217A1.

    CFTR correctors (Compounds A to F) promote the rescue of R98H mutant of alpha-sarcoglycan in HEK293 cell model. Alpha-sarcoglycan (α-SG) protein level has been determined by western blot (a representative experiment is shown in the top panel) on total protein content purified from cells expressing the R98H mutant treated with either CFTR correctors (compound A, B, C, D, E and F as indicated), MG132 (proteasome inhibitor) used as positive control, or correctors vehicle (DMSO) used as negative con
    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    KM11060 is a corrector of the F508 deletion (F508del)-cystic fibrosis transmembrane conductance regulator (CFTR) trafficking defect. KM11060 can be used for the research of F508del-CFTR processing defect and development of cystic fibrosis research[1].

    體外研究
    (In Vitro)

    Small-molecule correctors such as KM11060 may serve as useful pharmacological tools in studies of the F508del-CFTR processing defect and in the development of cystic fibrosis therapeutics. KM11060 rescues F508del-CFTR trafficking in cultured cells and native epithelial tissues. KM11060 partially corrects F508del-CFTR processing and increases surface expression to 75% of that observed in cells incubated at low temperature. Up to 50% of the F508del-CFTR in cells treated with KM11060 was complex-glycosylated, indicating passage through the Golgi. KM11060 as a promising compound for further development of CF therapeutics. [1]

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

    體內(nèi)研究
    (In Vivo)

    In LPS-induced acute lung inflammation, blockade of PSGL-1 (P-selectin glycoprotein ligand-1) or P-selectin, antagonism of PAF by WEB2086, or correction of mutated CFTR trafficking by KM11060 could significantly increase plasma lipoxin A4 levels in F508del relevant to wildtype mice. [2]

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

    分子量

    422.33

    Formula

    C19H17Cl2N3O2S

    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 : 50 mg/mL (118.39 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 2.3678 mL 11.8391 mL 23.6782 mL
    5 mM 0.4736 mL 2.3678 mL 4.7356 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    90% Corn Oil

      Solubility: ≥ 5 mg/mL (11.84 mM); 澄清溶液

      此方案可獲得 ≥ 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 50.0 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)。
    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, 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 2.3678 mL 11.8391 mL 23.6782 mL 59.1954 mL
    5 mM 0.4736 mL 2.3678 mL 4.7356 mL 11.8391 mL
    10 mM 0.2368 mL 1.1839 mL 2.3678 mL 5.9195 mL
    15 mM 0.1579 mL 0.7893 mL 1.5785 mL 3.9464 mL
    20 mM 0.1184 mL 0.5920 mL 1.1839 mL 2.9598 mL
    25 mM 0.0947 mL 0.4736 mL 0.9471 mL 2.3678 mL
    30 mM 0.0789 mL 0.3946 mL 0.7893 mL 1.9732 mL
    40 mM 0.0592 mL 0.2960 mL 0.5920 mL 1.4799 mL
    50 mM 0.0474 mL 0.2368 mL 0.4736 mL 1.1839 mL
    60 mM 0.0395 mL 0.1973 mL 0.3946 mL 0.9866 mL
    80 mM 0.0296 mL 0.1480 mL 0.2960 mL 0.7399 mL
    100 mM 0.0237 mL 0.1184 mL 0.2368 mL 0.5920 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:
    KM11060
    目錄號(hào):
    HY-19970
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