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  2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. RN486

RN486 是一種有效的，選擇性的，具有口服活性的 Btk 抑制劑，IC50 為 4.0 nM，Kd 為 0.31 nM，對(duì)其他激酶的活性較低。RN486 可用于類風(fēng)濕關(guān)節(jié)炎和系統(tǒng)性紅斑狼瘡的研究。

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RN486 Chemical Structure

RN486 Chemical Structure

CAS No. : 1242156-23-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1735
In-stock
1 mg ￥679
In-stock
5 mg ￥1300
In-stock
10 mg ￥2100
In-stock
25 mg ￥4200
In-stock
50 mg 現(xiàn)貨 詢價(jià)
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

    RN486 purchased from MCE. Usage Cited in: Blood Adv. 2020 Jun 9;4(11):2439-2450.  [Abstract]

    Western blot on whole-cell lysates from B cells with indicated genotype (wild-type or C481S), inhibitor treatment (ibrutinib or RN486) and stimulation (anti-IgM and H2O2).

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research[1][2][3].

    IC50 & Target

    IC50: 4.0 nM (Btk)[1]
    Kd: 0.31 nM (Btk)[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Ramos IC50
    27 nM
    Compound: RN486
    Inhibition of BTK in human Ramos cells assessed as reduction in IgM-induced calcium influx incubated for 20 mins by Fluo-4 dye based fluorescence assay
    Inhibition of BTK in human Ramos cells assessed as reduction in IgM-induced calcium influx incubated for 20 mins by Fluo-4 dye based fluorescence assay
    		[PMID: 25515957]
    Ramos IC50
    27.3 nM
    Compound: 3, RN486
    Inhibition of BTK in human Ramos cells after 20 mins by fluorescence assay
    Inhibition of BTK in human Ramos cells after 20 mins by fluorescence assay
    		[PMID: 25596757]
    體外研究
    (In Vitro)

    RN486 blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21 nM)[1].
    In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which is dose-dependently blocked by RN486[2].

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

    RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 (1-30 mg/kg) inhibits both joint and systemic inflammation, reducing both paw swelling and inflammatory markers in the blood[1].

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

    606.69

    Formula

    C35H35FN6O3
    CAS 號(hào)
    性狀

    固體

    顏色

    Off-white to light yellow

    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 : 24 mg/mL (39.56 mM; 超聲加熱助溶; 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 1.6483 mL 8.2414 mL 16.4829 mL
    5 mM 0.3297 mL 1.6483 mL 3.2966 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(guò)程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 99.87%

    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 1.6483 mL 8.2414 mL 16.4829 mL 41.2072 mL
    5 mM 0.3297 mL 1.6483 mL 3.2966 mL 8.2414 mL
    10 mM 0.1648 mL 0.8241 mL 1.6483 mL 4.1207 mL
    15 mM 0.1099 mL 0.5494 mL 1.0989 mL 2.7471 mL
    20 mM 0.0824 mL 0.4121 mL 0.8241 mL 2.0604 mL
    25 mM 0.0659 mL 0.3297 mL 0.6593 mL 1.6483 mL
    30 mM 0.0549 mL 0.2747 mL 0.5494 mL 1.3736 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：
    RN486
    目錄號(hào)：
    HY-18018
    需求量：