1. GPCR/G Protein
  2. G protein-coupled Bile Acid Receptor 1
  3. INT-777

INT-777  (Synonyms: S-EMCA)

目录号: HY-15677 纯度: ≥98.0%
COA 产品使用指南

INT-777是有效的 TGR5 激动剂,EC50 为 0.82 μM。

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INT-777 Chemical Structure

INT-777 Chemical Structure

CAS No. : 1199796-29-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3470
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2 mg ¥2333
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5 mg ¥3500
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10 mg ¥5000
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 29 篇科研文献

WB
IHC

    INT-777 purchased from MCE. Usage Cited in: J Am Soc Nephrol. 2018 Nov;29(11):2658-2670.  [Abstract]

    Western blots show that INT-767, INT-777, and INT747 upregulate AQP2 protein expression.

    INT-777 purchased from MCE. Usage Cited in: Front Immunol. 2018 Oct 2;9:2289.  [Abstract]

    Immunoblot analysis of p-IRF3 and p-AKT in lysates of peritoneal macrophages (PEMs) pretreated with MK2206 (3 μM) or INT-777 (500 μM) for 1 h, and then infected with vesicular stomatitis virus (VSV) for 8 h.

    INT-777 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 3;503(1):38-44.  [Abstract]

    Western Blot analysis of RIP3, and p-MLKL protein expressions detected in pancreatic tissues with the treatment of AP or AP plus INT-777.

    INT-777 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 3;503(1):38-44.  [Abstract]

    Representative immunohistochemistry images for RIP3 expression in the pancreas with the treatment of AP or AP plus INT-777.

    INT-777 purchased from MCE. Usage Cited in: Chinese Journal of Pathophysiology. 2017, 33(2):239-243.

    The effects of TGR5 activation on the mRNA (A) and protein (B) expression of CaN in the mouse cardiomyocytes induced by high glucose (HG).

    INT-777 purchased from MCE. Usage Cited in: Immunity. 2016 Oct 18;45(4):944.  [Abstract]

    INT-777, a semi-synthetic TGR5 agonist, markedly represses caspase-1 maturation and IL-1β or IL-18 but not the TNF-α secretion induced by Nigericin, similar to LCA. LPS-primed BMDMs are treated with different doses of INT-777 and then stimulated with Nigericin. Supernatants (SN) and cell extracts (Lysate) are analyzed by immunoblotting.

    INT-777 purchased from MCE. Usage Cited in: Endocrine. 2016 Dec;54(3):657-670.  [Abstract]

    After the transfection, the GMCs are treated with 10 μM INT-777 or DMSO (control) upon HG stimulation for 24 h. Western blot is performed to measure the protein expressions of FN and TGF-β. Upon HG stimulation, INT-777 treatment alone can significantly reduce the FN and TGF-β1 protein expressions, and the effect is potentiated by TGR5 overexpression.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM[1].

    IC50 & Target

    EC50: 0.82 μM (TGR5)[1]

    体外研究
    (In Vitro)

    INT-777 是一种新型强效选择性 TGR5 激动剂,具有显著的体内活性[1]
    INT-777 (3 μM) 以 cAMP 依赖性方式增加人肠内分泌细胞系 NCI-H716 中 ATP 的产生[2]
    将 INT-777 (10 μM) 添加到浆膜剥离的远端结肠段的浆膜侧时,可降低 Isc 并增加 TEER。在无神经元和经 TTX 处理的粘膜-粘膜下层制剂中,INT-777 对基础分泌的影响降低[3]

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

    体内研究
    (In Vivo)

    INT-777 (1 μM/min/kg,口服) 具有强利胆作用,可防止羧基 CoA 激活和随后的结合,从而有利于其胆肝分流通路,在 HF 喂养的 TGR5-Tg 雄性中具有导管吸收和强利胆作用小鼠[1]。INT-777 (30 mg/kg/天,口服) 在 TGR5-Tg 小鼠中增加能量消耗并减少高脂肪喂养时的肝脂肪变性和肥胖[2]

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

    分子量

    450.65

    Formula

    C27H46O5

    CAS 号
    性状

    固体

    颜色

    White to yellow

    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 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    Ethanol 中的溶解度 : ≥ 50 mg/mL (110.95 mM)

    DMSO 中的溶解度 : ≥ 31 mg/mL (68.79 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 2.2190 mL 11.0951 mL 22.1902 mL
    5 mM 0.4438 mL 2.2190 mL 4.4380 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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

    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% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.55 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。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.55 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。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 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。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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: 0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (11.10 mM); Suspension solution; 超声助溶

    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

    纯度: 100.0%

    参考文献
    Cell Assay
    [2]

    The experiments are carried out in STC-1 or NCI-H716 cells treated with vehicle (DMSO) or INT-777. INT-777 is assessed for its agonistic activity on TGR5. cAMP production is performed. Cytochrome C oxidase activity is evaluated by following the oxidation of fully reduced cytochrome C at 550 nm. ATP/ADP ratio and GLP-1 release is measured according to the manufacturer's instruction. Primary brown adipocytes are prepared and ileal explants are prepared.

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

    Animal Administration
    [2]

    Age-matched male mice are used for all experiments. Genetically engineered mouse models (GEMMs), i.e. TGR5-Tg and TGR5-/- mice are generated. Diet-induced obesity (DIO) in the GEMMs or C57BL/6J mice is induced by feeding 8-week-old mice with a HF-diet (60%Cal/fat, D12492) for at least 8 weeks, as mentioned in the text and figure legends. In the dietary intervention experiments, INT-777 is mixed with diet at the dose sufficient to reach an in vivo dose of 30mg/kg/d. Mouse phenotyping experiments are performed according to EMPRESS protocols and aimed to assess food and water intake, body composition, energy expenditure, glucose and lipid homeostasis, and plasma biochemistry.

    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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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 / Ethanol 1 mM 2.2190 mL 11.0951 mL 22.1902 mL 55.4754 mL
    5 mM 0.4438 mL 2.2190 mL 4.4380 mL 11.0951 mL
    10 mM 0.2219 mL 1.1095 mL 2.2190 mL 5.5475 mL
    15 mM 0.1479 mL 0.7397 mL 1.4793 mL 3.6984 mL
    20 mM 0.1110 mL 0.5548 mL 1.1095 mL 2.7738 mL
    25 mM 0.0888 mL 0.4438 mL 0.8876 mL 2.2190 mL
    30 mM 0.0740 mL 0.3698 mL 0.7397 mL 1.8492 mL
    40 mM 0.0555 mL 0.2774 mL 0.5548 mL 1.3869 mL
    50 mM 0.0444 mL 0.2219 mL 0.4438 mL 1.1095 mL
    60 mM 0.0370 mL 0.1849 mL 0.3698 mL 0.9246 mL
    Ethanol 80 mM 0.0277 mL 0.1387 mL 0.2774 mL 0.6934 mL
    100 mM 0.0222 mL 0.1110 mL 0.2219 mL 0.5548 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:
    INT-777
    目录号:
    HY-15677
    需求量: