2. GPCR/G Protein
  3. Free Fatty Acid Receptor
  4. Fasiglifam

Fasiglifam  (Synonyms: TAK-875)

目录号: HY-10480 纯度: 98.94%
COA 产品使用指南

摩尔计算器

Fasiglifam (TAK-875) 是一种有效的，可口服的，具有选择性的 GPR40 激动剂，EC50 值为 72 nM。

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Fasiglifam Chemical Structure

Fasiglifam Chemical Structure

CAS No. : 1000413-72-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1210
In-stock
2 mg ￥800
In-stock
5 mg ￥1100
In-stock
10 mg ￥2100
In-stock
50 mg ￥4700
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Fasiglifam:

Fasiglifam 相关抗体

Top Publications Citing Use of Products

    Fasiglifam purchased from MCE. Usage Cited in: PLoS One. 2018 Jul 11;13(7):e0200449.  [Abstract]

    TAK-875 increases (p<0.05) the membrane expression of FFAR1 compared to the untreated control by 97%.

    Fasiglifam purchased from MCE. Usage Cited in: J Cell Biochem. 2017 May;118(5):1249-1261.  [Abstract]

    Free fatty acid receptor 1 (FFAR1) agonist induces LOX-1 upregulation in cultured vascular smooth muscle cells (VSMCs). Cultured VSMCs are treated with synthetic agonists for either FFAR1 (TAK-875) or FFAR4 (TUG-891) at indicated doses for 24 hours. Both FFAR1 and FFAR4 are known responsible for long chain fatty acids. 0.1% DMSO is used as solvent control (SC). Western blotting detection indicates that treatment with agonistic action of FFAR1, but not FFAR4, remarkably upregulated LOX-1 expressi

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.

    IC50 & Target

    EC50: 72 nM (GPR40)
    体外研究
    (In Vitro)

    Fasiglifam (TAK-875) (0.01-10 μM) produces a concentration-dependent increase in intracellular IP production in CHO-hGPR40, with EC50 of 0.072 μM. Fasiglifam (TAK-875) (0.1-10 μM) dose-dependently augments intracellular IP production in CHO cells[1]. Fasiglifam (TAK-875) (3-30 μM) concentration-dependently augments [Ca2+]i. In the presence of 10 mM glucose, TAK-875 (0.001-10 μM) dose-dependently stimulats insulin secretion from INS-1 833/15 cells[2].

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

    Fasiglifam 相关抗体:
    体内研究
    (In Vivo)

    Fasiglifam (TAK-875) (10 mg/kg, p.o.) increases plasma insulin levels in ZDF rats. Fasiglifam (TAK-875) (30 mg/kg, p.o.) improves fasting hyperglycemia without affecting fasting normoglycemia. Fasiglifam (TAK-875) at 30 mg/kg, which is a 3- to 10-fold higher dose compared with the dose that improved glucose tolerance in diabetic rats, does not alter fasting glucose levels in SD rats with normal glucose homeostasis. Likewise, Fasiglifam (TAK-875) does not significantly alter insulin secretion in SD rats with normal fasting glucose levels [1].

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

    524.63

    Formula

    C29H32O7S
    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
    细胞实验： 

    DMSO 中的溶解度 : ≥ 128 mg/mL (243.98 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 1.9061 mL 9.5305 mL 19.0611 mL
    5 mM 0.3812 mL 1.9061 mL 3.8122 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

    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: ≥ 2.5 mg/mL (4.77 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (4.77 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：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

    只
    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

    纯度: 98.94%

    COA (167 KB) LCMS (259 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    INS-1 832/13 cells are suspended in RPMI medium and seeded in a 96-well plate at a density of 2×104 cells/well; 1% BSA and 0.1% DMSO alone (control), palmitic acid (10, 100, and 1000 μM), oleic acid (10, 100, and 1000 μM), or Fasiglifam (TAK-875: 1, 10, and 100 μM) is added to the plate. After 72-h culture, medium is discarded, and cells are preincubated for 2 h with KRBH containing 1 mM glucose and 0.2% BSA at 37°C. After discarding of the preincubation buffer, KRBH containing 1 or 20 mM glucose and 0.2% BSA is added, and the plate is further incubated for 2 h. The insulin concentration in the supernatant is measured as described above. To measure intracellular insulin content, INS-1 832/13 cells are exposed to 1% BSA and 0.1% DMSO alone (control), palmitic acid (1000 μM), oleic acid (1000 μM), or Fasiglifam (TAK-875) (100 μM) with 1% BSA and 0.1% DMSO. After incubation, cells are washed once with phosphate-buffered saline, and acid-ethanol solution is added to each well, followed by sonication on ice. Intracellular insulin is extracted by overnight incubation at −30°C, followed by separation of supernatant by centrifugation at 12,000 rpm×5 min at 4°C.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    At 18 weeks of age, the N-STZ-1.5 rats are fasted overnight and orally given vehicle (0.5% methylcellulose) or Fasiglifam (TAK-8751, 3, and 10 mg/kg). Sixty minutes later, all animals receive an oral glucose load (1 g/kg). Blood samples are collected from the tail vein before drug administration, before glucose load (time 0), and 10, 30, 60, and 120 min after the glucose load. Plasma glucose and insulin levels are measured with an AutoAnalyzer 7080 and radioimmunoassay, respectively. To see the effects of Fasiglifam (TAK-875) on fasting normoglycemia and hyperglycemia, SD rats (8 weeks old) or ZDF and ZL rats (12 weeks old) are fasted overnight and orally given vehicle (0.5% methylcellulose), Fasiglifam (TAK-875) (10 or 30 mg/kg), nateglinide (50 mg/kg), or glibenclamide (10 mg/kg). Blood samples are collected from the tail vein before drug administration (time 0) and 0.5, 1, 2, and 3 h (SD rats) and 0.5, 1, 2, 4, and 6 h (ZDF and ZL rats) after drug administration, and plasma glucose and insulin levels are measured as described above.

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

    Fasiglifam 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 1.9061 mL 9.5305 mL 19.0611 mL 47.6526 mL
    5 mM 0.3812 mL 1.9061 mL 3.8122 mL 9.5305 mL
    10 mM 0.1906 mL 0.9531 mL 1.9061 mL 4.7653 mL
    15 mM 0.1271 mL 0.6354 mL 1.2707 mL 3.1768 mL
    20 mM 0.0953 mL 0.4765 mL 0.9531 mL 2.3826 mL
    25 mM 0.0762 mL 0.3812 mL 0.7624 mL 1.9061 mL
    30 mM 0.0635 mL 0.3177 mL 0.6354 mL 1.5884 mL
    40 mM 0.0477 mL 0.2383 mL 0.4765 mL 1.1913 mL
    50 mM 0.0381 mL 0.1906 mL 0.3812 mL 0.9531 mL
    60 mM 0.0318 mL 0.1588 mL 0.3177 mL 0.7942 mL
    80 mM 0.0238 mL 0.1191 mL 0.2383 mL 0.5957 mL
    100 mM 0.0191 mL 0.0953 mL 0.1906 mL 0.4765 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.

    Keywords:

    Fasiglifam1000413-72-8TAK-875TAK875TAK 875Free Fatty Acid ReceptorFFARInhibitorinhibitorinhibit

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