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

INT-777是有效的 TGR5 激動(dòng)劑，EC50 為 0.82 μM。

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INT-777 Chemical Structure

INT-777 Chemical Structure

CAS No. : 1199796-29-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥3470
In-stock
2 mg ￥2333
In-stock
5 mg ￥3500
In-stock
10 mg ￥5000
In-stock
50 mg   詢價(jià)  
100 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of INT-777:

MCE 顧客使用本產(chǎn)品發(fā)表的 36 篇科研文獻(xiàn)

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

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO EC50
    3.44 μM
    Compound: 8, S-EMCA, INT-777
    Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
    Agonist activity at human TGR5 expressed in CHO cells assessed as increase in CRE-driven gene expression by luciferase reporter gene assay
    		[PMID: 20014870]
    COS-1 EC50
    > 100 μM
    Compound: 8, S-EMCA, INT-777
    Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay
    Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay
    		[PMID: 20014870]
    HEK293 EC50
    0.36 μM
    Compound: 1, INT-777, S-EMCA
    Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
    Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
    		[PMID: 24007860]
    HEK293 EC50
    1.23 μM
    Compound: 1, INT-777, S-EMCA
    Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
    Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
    		[PMID: 24007860]
    HEK293 EC50
    293 nM
    Compound: INT-777
    Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
    Agonist activity at human TGR5 expressed in HEK293 cells assessed as cAMP level after 48 hrs by fluorescent assay
    		[PMID: 25082126]
    NCI-H716 EC50
    0.82 μM
    Compound: 3, INT-777, S-EMCA
    Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
    Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis
    		[PMID: 24900463]
    體外研究
    (In Vitro)

    INT-777 是一種新型強(qiáng)效選擇性 TGR5 激動(dòng)劑，具有顯著的體內(nèi)活性[1]。
    INT-777 (3 μM) 以 cAMP 依賴性方式增加人腸內(nèi)分泌細(xì)胞系 NCI-H716 中 ATP 的產(chǎn)生[2]。
    將 INT-777 (10 μM) 添加到漿膜剝離的遠(yuǎn)端結(jié)腸段的漿膜側(cè)時(shí)，可降低 Isc 并增加 TEER。在無神經(jīng)元和經(jīng) TTX 處理的粘膜-粘膜下層制劑中，INT-777 對(duì)基礎(chǔ)分泌的影響降低[3]。

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

    INT-777 (1 μM/min/kg，口服) 具有強(qiáng)利膽作用，可防止羧基 CoA 激活和隨后的結(jié)合，從而有利于其膽肝分流通路，在 HF 喂養(yǎng)的 TGR5-Tg 雄性中具有導(dǎo)管吸收和強(qiáng)利膽作用小鼠[1]。INT-777 (30 mg/kg/天，口服) 在 TGR5-Tg 小鼠中增加能量消耗并減少高脂肪喂養(yǎng)時(shí)的肝脂肪變性和肥胖[2]。

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

    450.65

    Formula

    C27H46O5
    CAS 號(hào)
    性狀

    固體

    顏色

    White to 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 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    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)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.55 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 EtOH 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.55 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 EtOH 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (11.10 mM); Suspension solution; 超聲助溶

    掃碼獲得
    動(dòng)物溶解方案

    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)過程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， PEG300/PEG400，Tween 80，均可在 MCE 網(wǎng)站選購。
    純度 & 產(chǎn)品資料

    純度: 100.0%

    參考文獻(xiàn)
    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.
    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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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 / 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

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    產(chǎn)品名稱：
    INT-777
    目錄號(hào)：
    HY-15677
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