1. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  2. JAK
  3. Baricitinib phosphate

Baricitinib phosphate  (Synonyms: 磷酸巴瑞克替尼; LY3009104 phosphate; INCB028050 phosphate)

目录号: HY-15315A 纯度: 99.97%
COA 产品使用指南 技术支持

Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) 是一种选择性的,可口服的 JAK1/JAK2 抑制剂,IC50 值分别为 5.9 nM 和 5.7 nM。

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Baricitinib phosphate Chemical Structure

Baricitinib phosphate Chemical Structure

CAS No. : 1187595-84-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥516
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2 mg ¥350
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5 mg ¥500
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10 mg ¥700
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100 mg ¥2200
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Customer Review

Other Forms of Baricitinib phosphate:

MCE 顾客使用本产品发表的 50 篇科研文献

WB

    Baricitinib phosphate purchased from MCE. Usage Cited in: RSC Adv. 2018, 8, 21534-21540.

    M14 and A2058 cells are treated with IFN-γ (10 ng/mL) after Lac (100 μg/mL) or baricitinib (0.5 μM) for the indicated times. Whole cell lysates are subjected to western blotting.

    Baricitinib phosphate purchased from MCE. Usage Cited in: Institute of Natural Medicine,University of Toyama, Japan. 2018, Nov.

    Western analysis of pJAK2, JAK2, pSTAT1, STAT1 and IRF1 protein in M14 and A2058 cells treated with IFN-g (10 ng/mL) after Lac (100 μg/mL) or baricitinib (0.5 μM) for the indicated times.

    Baricitinib phosphate purchased from MCE. Usage Cited in: PLoS One. 2017 Jul 14;12(7):e0181126.  [Abstract]

    An activator of Stat3, colivelin (0.1 or 1 µM), rescued Baricitinib-induced RANKL down-regulation in osteoblast cultures.

    查看 JAK 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.

    IC50 & Target[1]

    JAK2

    5.7 nM (IC50)

    JAK1

    5.9 nM (IC50)

    Tyk2

    53 nM (IC50)

    JAK3

    560 nM (IC50)

    体外研究
    (In Vitro)

    在基于细胞的实验中,Baricitinib phosphate (INCB028050 phosphate) 被证明是一种有效的 JAK 信号传导和功能抑制剂。在 PBMCs 中,Baricitinib 抑制 IL -6 刺激的标准底物 STAT3 (pSTAT3) 的磷酸化和随后趋化因子 MCP-1 的产生,IC50 值分别为 44 nM 和 40 nM。在分离的幼稚 T 细胞中,INCB028050 也抑制 IL-23 刺激的 pSTAT3 (IC50=20 nM)。重要的是,这种抑制阻止了 Th17 细胞产生的两种致病细胞因子 (IL-17IL-22) 的产生,Th17 细胞是辅助性 T 细胞的一种亚型,具有明显的炎症和致病特性,IC50 值为 50 nM。与之形成鲜明对比的是,结构相似但无效的 JAK1/2抑制剂 INCB027753 和 INCB029843 在浓度高达 10 μM时,在这些检测系统中都没有显著影响[1]

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

    体内研究
    (In Vivo)

    Baricitinib phosphate (INCB028050 phosphate) 处理与对照体相比,在 2 周的治疗期间,以 1 mg/kg 的剂量抑制后肢体积的增加 50%,以 3 或 10 mg/kg 的剂量抑制后肢体积的增加 95%。因为基线脚爪体积测量是在治疗第 0 天进行的——在有明显疾病迹象的动物中——所以在肿胀明显改善的动物中,有可能 >100% 抑制[1]
    通过 H&E 染色评估,Baricitinib (0.7 mg/天) 处理的小鼠与对照处理的小鼠相比,炎症明显减轻,CD8 浸润减少,MHC I 类和 II 类表达减少。CD8+NKG2D+ 细胞是小鼠和人类斑秃 (AA) 疾病的关键效应因子,与对照小鼠相比,Baricitinib 治疗小鼠的 CD8+NKG2D+ 细胞显著减少[2]

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

    Clinical Trial
    分子量

    469.41

    同用名

    磷酸巴瑞克替尼; LY3009104 phosphate; INCB028050 phosphate

    Formula

    C16H20N7O6PS

    CAS 号
    性状

    固体

    颜色

    White to yellow

    中文名称

    磷酸巴瑞克替尼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

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

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 4.7 mg/mL (10.01 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1303 mL 10.6517 mL 21.3033 mL
    5 mM 0.4261 mL 2.1303 mL 4.2607 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.43 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.43 mM); 悬浊液; 超声助溶

      此方案可获得 2.08 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

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

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.97%

    参考文献
    Cell Assay
    [1]

    For the determination of IL-6-induced MCP-1 production, PBMCs are plated at 3.3×105 cells per well in RPMI 1640+10% FCS in the presence or absence of various concentrations of INCB028050 (1 nM, 10 nM, 100 nM, 1 μM, and 10 μM). Following preincubation with compound for 10 min at room temperature, cells are stimulated by adding 10 ng/mL human recombinant IL-6 to each well. Cells are incubated for 48 h at 37°C, 5% CO2. Supernatants are harvested and analyzed by ELISA for levels of human MCP-1. The ability of INCB028050 to inhibit IL-6-induced secretion of MCP-1 is reported as the concentration required for 50% inhibition (IC50). Proliferation of Ba/F3-TEL-JAK3 cells is performed over 3 d using Cell-Titer Glo[1].

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

    Animal Administration
    [1][2]

    Rats[1]
    Female rats (n=6 per gender per group) are given a dose of 10 mg/kg Baricitinib and given by oral gavage at 10 mL/kg. The first three rats are bled at 0 (predose), 2, 8, and 24 h, and the second three rats are bled 1, 4, and 12 h after dosing. EDTA is used as the anticoagulant, and samples are centrifuged to obtain plasma. An analytical method for the quantification of INCB028050 has been developed and used to analyze samples from toxicology studies. The method combines a protein precipitation extraction with 10% methanol in acetonitrile and LC/MS/MS analysis. The method has demonstrated a linear assay range 1-5000 nM using 0.1 mL of study samples. Data are processed using Analyst 1.3.1. A standard curve is determined from peak area ratio versus concentration using a weighted linear regression (1/x2).
    Mice[2]
    The C3H/HeJ graft-recipient mouse model of AA is used for these experiments. Briefly, alopecic skin from a C3H/HeJ mouse that spontaneously developed hair loss is grafted onto 8-10 week old C3H/HeJ mice free of disease. At the time of grafting, an osmotic pump that administered approximately 0.7 mg/day of Baricitinib or placebo is implanted. Osmotic pumps are changed monthly. A time-to-event survival analysis for interval censored data is performed. The survival and interval packages in R are used to perform log-rank tests. The hypothesis that the survival distributions are equal in the (n=10) Baricitinib-treated mice and (n=10) placebo-treated mice is rejected at the 5% level using Sun's score to perform an exact log-rank two-sample test with the p-value of 0.0035.

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

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1303 mL 10.6517 mL 21.3033 mL 53.2583 mL
    5 mM 0.4261 mL 2.1303 mL 4.2607 mL 10.6517 mL
    10 mM 0.2130 mL 1.0652 mL 2.1303 mL 5.3258 mL
    Help & FAQs
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      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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