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

INT-777 est un puissant agoniste de TGR5 avec un EC50 de 0,82 μM.

INT-777 ist ein potenter TGR5-Agonist mit einer EC50 von 0,82 uM.

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

For research use only. We do not sell to patients.

INT-777 Chemical Structure

INT-777 Chemical Structure

CAS No. : 1199796-29-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 462 In-stock
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Solid
5 mg USD 420 In-stock
10 mg USD 600 In-stock
50 mg USD 1800 In-stock
100 mg USD 2520 In-stock
200 mg   Get quote  
500 mg   Get quote  

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

Customer Review

Based on 36 publication(s) in Google Scholar

Other Forms of INT-777:

Top Publications Citing Use of Products

29 Publications Citing Use of MCE INT-777

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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    EC50: 0.82 μM (TGR5)[1]

    In Vitro

    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.

    In Vivo

    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.

    Molecular Weight

    450.65

    Formula

    C27H46O5

    CAS No.
    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    Ethanol : ≥ 50 mg/mL (110.95 mM)

    DMSO : ≥ 31 mg/mL (68.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    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
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

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

      Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (11.10 mM); Suspension solution; Need ultrasonic

    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.
    Purity & Documentation

    Purity: 100.0%

    References
    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.

    References

    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
    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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    INT-777 Related Classifications

    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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    Product Name:
    INT-777
    Cat. No.:
    HY-15677
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