1. GPCR/G Protein
  2. G protein-coupled Bile Acid Receptor 1
  3. SB756050

SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.

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CAS. Nr. : 447410-57-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    SB756050 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2020 Jul 6;6:56.  [Abstract]

    GES-1 cells are treated with SB756050 (2, 5, and 10 μM) for 24 h. KLF4 and CDX2 protein expression is examined by WB. The results show that KLF4 and CDX2 expression is significantly increased.
    • Biologische Aktivität

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    Beschreibung

    SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.

    In Vitro

    TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D)[1].

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

    In Vivo

    SB756050 is well‐tolerated; it is readily absorbed, exhibited nonlinear pharmacokinetics with a less than dose‐proportional increase in plasma exposure above 100 mg, and demonstrates no significant changes in exposure when co‐administered with sitagliptin. SB756050 demonstrates highly variable pharmacodynamic effects both within dose groups and between doses, with increases in glucose seen at the two lowest doses and no reduction in glucose seen at the two highest doses. The glucose effects of SB756050 sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different[1].

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

    Klinische Studie
    Molekulargewicht

    500.59

    Formel

    C21H28N2O8S2

    CAS. Nr.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S(N1CCN(S(=O)(C2=CC=C(OC)C(OC)=C2)=O)CCC1)(C3=CC=C(OC)C(OC)=C3)=O

    Versand

    Room temperature in continental US; may vary elsewhere.

    Speicherung
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : 50 mg/mL (99.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9976 mL 9.9882 mL 19.9764 mL
    5 mM 0.3995 mL 1.9976 mL 3.9953 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molaritätsrechner

    • Verdünnungsrechner

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Reinheit & Dokumentation

    Purity: 99.75%

    Verweise

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9976 mL 9.9882 mL 19.9764 mL 49.9411 mL
    5 mM 0.3995 mL 1.9976 mL 3.9953 mL 9.9882 mL
    10 mM 0.1998 mL 0.9988 mL 1.9976 mL 4.9941 mL
    15 mM 0.1332 mL 0.6659 mL 1.3318 mL 3.3294 mL
    20 mM 0.0999 mL 0.4994 mL 0.9988 mL 2.4971 mL
    25 mM 0.0799 mL 0.3995 mL 0.7991 mL 1.9976 mL
    30 mM 0.0666 mL 0.3329 mL 0.6659 mL 1.6647 mL
    40 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 mL
    50 mM 0.0400 mL 0.1998 mL 0.3995 mL 0.9988 mL
    60 mM 0.0333 mL 0.1665 mL 0.3329 mL 0.8324 mL
    80 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 mL
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    • 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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    Produktname:
    SB756050
    Art. -Nr.:
    HY-102016
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