1. GPCR/G Protein Neuronal Signaling
  2. GPR119
  3. MBX-2982

MBX-2982 是一种口服选择性的 G 蛋白偶联受体 119 (GPR119) 激动剂。

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MBX-2982 Chemical Structure

MBX-2982 Chemical Structure

CAS No. : 1037792-44-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1490
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1 mg ¥613
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5 mg ¥1350
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10 mg ¥2280
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50 mg ¥7800
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100 mg   询价  
200 mg   询价  

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Top Publications Citing Use of Products

    MBX-2982 purchased from MCE. Usage Cited in: Patent. US9895370B2.

    When the GPR119 ligand (MBX-2982) is time-dependently treated, AMPK is highly activated (AMPK and ACC phosphorylation).

    MBX-2982 purchased from MCE. Usage Cited in: FASEB J. 2016 Jan;30(1):324-35.  [Abstract]

    Treatment with 2 synthetic GPR119 agonists, MBX-2982 (MBX) and GSK1292263 (GSK), suppresses T090-induced SREBP-1 expression and mRNA levels of SREBP-1 target genes such as FAS, ACC, and SCD-1.

    MBX-2982 purchased from MCE. Usage Cited in: College of Pharmacy. Seoul National University. 2015 Aug.

    Effects of GPR119 ligands on T090-induced pSREBP-1 and lipogenic enzymes expression. Primary cultured hepatocytes from GPR119-WT and -KO mice and HepG2 cells are pretreated with two GPR119 ligands (MBX-2982 or GSK1292263) for 30 min and the cells are exposed to T090 for 12 h.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.

    IC50 & Target

    GPR119[1]

    体外研究
    (In Vitro)

    在“慢性孵育/清洗”实验中用 MBX-2982 (1 μM) 预处理细胞,与对照细胞相比,IBMX 包涵体捕获的 cAMP 积累显着增加(P<0.01;ANOVA;n=3-6),尽管广泛洗涤以去除多余的激动剂。AR-231,453 在与急性刺激观察到的相似的浓度范围内产生持续反应(1.82 倍变化),pEC50 分别为 8.67±0.11 和 8.93±0.17。同样,观察到 MBX-2982 的浓度反应发生较大但不太严重的变化(57.54 倍),持续和急性 pEC50 分别为 7.03±0.13 和 8.79±0.12[1]

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

    体内研究
    (In Vivo)

    为了检查 GLUTag 和原代肠细胞中的观察结果是否具有生理相关性,用 10 mg/kg 的 GPR119 激动剂 MBX-2982 处理 C57BL/6 小鼠。 请注意,为了检查直接的 GPR119 效应,本实验中没有联合使用 DPP-IV 抑制剂,而是使用 DPP-IV 抑制剂来保存血液样本中的活性 GLP-1。 给药 MBX-2982 的小鼠的血浆 GLP-1 水平在没有葡萄糖负荷的情况下增加,表明 GPR119 介导的 GLP-1 分泌不依赖于葡萄糖[2]

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

    Clinical Trial
    分子量

    448.54

    Formula

    C22H24N8OS

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (111.47 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2295 mL 11.1473 mL 22.2946 mL
    5 mM 0.4459 mL 2.2295 mL 4.4589 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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

    In Vivo:

    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    90% Corn Oil

      Solubility: ≥ 2.75 mg/mL (6.13 mM); 澄清溶液

      此方案可获得 ≥ 2.75 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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)。
    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
    参考文献
    Kinase Assay
    [1]

    HEK-GPR119 cells are transfected with GloSensor 22F plasmid and used for dynamic cAMP measurements 24-30 h later. Cell suspensions are made by dislodging the cells using PBS wash and Accutase treatment followed by resuspension in culture media. Cells are then washed twice by pelleting through centrifugation (300g, 5 min) and resuspension in assay buffer (Hank's Balanced Salt Solution supplemented with 20 mM HEPES and 0.01% fatty acid free BSA, pH 7.4). Cells are then counted and diluted to 600,000 cells/mL in buffer, before GloSensor cAMP reagent is added (2% v/v) and equilibrated with the cells for 2 h at 20°C with periodic mixing. 50 µl/well of cells are added to white-bottomed 384 well plates (30,000 cells/well) in triplicate and baseline luminescence is measuring using an Envision plate-reader. 5 μL of MBX-2982 (serially diluted in DMSO and then diluted 1:100 in assay buffer to obtain ×10 concentrated solution) is manually added to the assay wells to achieve the stated final concentration. Plates are incubated at 20°C with luminescence read at regular intervals to detect dynamic cAMP changes over time within the same wells. cAMP responses at each time-point are expressed as fold over control (vehicle-treated cells)[1].

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

    Cell Assay
    [1]

    HEK-GPR119 cells are grown to confluency in flasks, and cell suspensions are made by dislodging cells using PBS wash and accutase treatment followed by resuspension in culture media. Cells are then washed twice by pelleting through centrifugation (227g, 7 min, 20°C) and resuspension in warm assay buffer (Hank's Balanced Salt Solution supplemented with 20 mM HEPES and 0.01% fatty acid free BSA, pH 7.4), with a 5 min incubation at 37°C after the second wash. Cells are then counted and diluted to 200,000 cells/mL in warm assay buffer[1].

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

    Animal Administration
    [2]

    Mice[2]
    C57BL/6 male mice are used. Overnight fasted, 10 week-old male mice (n=20 per group) are given either vehicle (15% polyethylene glycol 400+85% of 23.5% hydroxypropyl-β-cyclodextrin) or MBX-2982 at 10 mg/kg via oral gavage. Half of the animals (n=10 per group) are killed by CO2 asphyxiation 30 min after compound dosing, and blood is collected by cardiac puncture. To preserve active GLP-1, a DPP-IV inhibitor (10 µL per 1 mL of blood) is pre-added to the blood collection tubes and, before the cardiac puncture, the walls of the syringes are rinsed with the DPP-IV inhibitor. The other half of the animals (n=10 per group) received a bolus of oral glucose (3 g/kg) 30 min after compound dosing, and are killed for blood collection 10 min after the glucose load. GLP-1 levels in the plasma samples are measured using the active GLP-1 (ver 2) kit.

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

    参考文献

    MBX-2982 相关分类

    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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2295 mL 11.1473 mL 22.2946 mL 55.7364 mL
    5 mM 0.4459 mL 2.2295 mL 4.4589 mL 11.1473 mL
    10 mM 0.2229 mL 1.1147 mL 2.2295 mL 5.5736 mL
    15 mM 0.1486 mL 0.7432 mL 1.4863 mL 3.7158 mL
    20 mM 0.1115 mL 0.5574 mL 1.1147 mL 2.7868 mL
    25 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2295 mL
    30 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8579 mL
    40 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3934 mL
    50 mM 0.0446 mL 0.2229 mL 0.4459 mL 1.1147 mL
    60 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9289 mL
    80 mM 0.0279 mL 0.1393 mL 0.2787 mL 0.6967 mL
    100 mM 0.0223 mL 0.1115 mL 0.2229 mL 0.5574 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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    产品名称:
    MBX-2982
    目录号:
    HY-15291
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