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

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

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1199796-29-6

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 462 在庫あり
Solution
10 mM * 1 mL in DMSO USD 462 在庫あり
Solid
5 mg $420 在庫あり
10 mg $600 在庫あり
25 mg $960 在庫あり
50 mg $1350 在庫あり
100 mg $1880 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 48 publication(s) in Google Scholar

Other Forms of INT-777:

Top Publications Citing Use of Products

顧客検証

WB
IHC

    INT-777 purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

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

    IC50 & Target

    EC50: 0.82 μM (TGR5)[1]

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    3.44 3
    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]
    CHO EC50
    3.44 3
    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]
    CHO EC50
    3.44 3
    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 3
    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]
    COS-1 EC50
    > 100 3
    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 3
    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]
    COS-1 EC50
    > 100 3
    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
    1.23 3
    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
    1.23 3
    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
    0.36 3
    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]
    NCI-H716 EC50
    13 3
    Compound: 1, INT-777
    Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
    Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
    [PMID: 23831134]
    HEK293 EC50
    293 1
    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 3
    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]
    NCI-H716 EC50
    0.82 3
    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]
    HEK293 EC50
    0.36 3
    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
    293 1
    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]
    HEK293 EC50
    1.23 3
    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 1
    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 3
    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]
    NCI-H716 EC50
    13 3
    Compound: 1, INT-777
    Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
    Agonist activity at GPBAR1 in human NCI-H716 cells assessed as stimulation of cAMP production
    [PMID: 23831134]
    体外実験

    INT-777 is a novel potent and selective TGR5 agonist with remarkable in vivo activity[1]. INT-777 (3 μM) increases ATP production in the human enteroendocrine cell line NCI-H716 in a cAMP-dependent manner[2]. INT-777 (10 μM) lowers Isc and increases TEER when added on the serosal side of seromuscular stripped distal colon segments. INT-777 effect on basal secretion is reduced in neuron-free and TTX-treated mucosal-submucosal preparations[3].

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

    体内実験

    INT-777 (1 μM/min/kg, p.o.) has a potent choleretic effect, prevents carboxyl CoA activation and subsequent conjugation, thereby favoring its chole-hepatic shunt pathway with a ductular absorption and a potent choleretic effect in HF-fed TGR5-Tg male mice[1]. INT-777 (30 mg/kg/day, p.o.) increases energy expenditure and reduces hepatic steatosis and obesity upon high-fat feeding in TGR5-Tg mice[2].

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

    分子量

    450.65

    分子式

    C27H46O5

    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O[C@@H]1CC[C@@]2(C)[C@@]([C@@H](CC)[C@@H](O)[C@]3([H])[C@]2([H])C[C@H](O)[C@@]4(C)[C@@]3([H])CC[C@@H]4[C@H](C)C[C@H](C)C(O)=O)([H])C1

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (221.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : ≥ 50 mg/mL (110.95 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2219 mL 1.1095 mL 2.2190 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

    C1

    ×
    体積 (開始)

    V1

    =
    濃度 (終了)

    C2

    ×
    体積 (終了)

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (11.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (11.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 100.0%

    参考文献
    細胞実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 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
    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
    C1   V1   C2   V2
    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.

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

     

    カスタマ需要量 *

    お名前 *

     

    タイトル

    メールアドレス *

     

    電話番号 *

    デパートメント

     

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

         

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    INT-777
    製品番号:
    HY-15677
    数量:
    MCE 日本正規代理店: