1. Membrane Transporter/Ion Channel
  2. SGLT
  3. Sotagliflozin

Sotagliflozin  (Synonyms: LX-4211; LP-802034)

Cat. No.: HY-15516 Pureza: 99.94%
Instrucciones de manejo Technical Support

Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Antidiabetic agents.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 1018899-04-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
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Revisión del cliente

Based on 13 publication(s) in Google Scholar

Other Forms of Sotagliflozin:

Top Publications Citing Use of Products

    Sotagliflozin purchased from MedChemExpress. Usage Cited in: J Nutr. 2020 Jul 1;150(7):1790-1798.  [Abstract]

    Effects of LX-4211 pretreatment on glucose-induced changes in protein expression in IECs of yellow catfish. Primary IECs are incubated in control or glucose (15 mM glucose) for 24 h with or without 2-h pretreatment with an SGLT1/2 dual inhibitor LX-4211 (20 μM).

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    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Antidiabetic agents.

    IC50 & Target

    SGLT1

     

    SGLT2

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    1.8 1
    Compound: 1
    Inhibition of human HA-tagged SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    Inhibition of human HA-tagged SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    [PMID: 28045524]
    HEK293 IC50
    1.8 1
    Compound: 1
    Inhibition of human HA-tagged SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    Inhibition of human HA-tagged SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    [PMID: 28045524]
    HEK293 IC50
    36.2 1
    Compound: 1
    Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    [PMID: 28045524]
    HEK293 IC50
    1.8 1
    Compound: 1
    Inhibition of human HA-tagged SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    Inhibition of human HA-tagged SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    [PMID: 28045524]
    HEK293 IC50
    36.2 1
    Compound: 1
    Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    [PMID: 28045524]
    HEK293 IC50
    36.2 1
    Compound: 1
    Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    Inhibition of human HA-tagged SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake measured after 1 to 2 hrs by scintillation counting method
    [PMID: 28045524]
    In Vitro

    LX4211 enhanced urinary glucose excretion by inhibiting SGLT2-mediated renal glucose reabsorption; markedly and significantly improved multiple measures of glycemic control, including fasting plasma glucose, oral glucose tolerance, and HbA(1c); and significantly lowered serum triglycerides. LX4211 also mediated trends for lower weight, lower blood pressure, and higher glucagon-like peptide-1 levels. In a follow-up single-dose study in 12 patients with T2DM, LX4211 (300 mg) significantly increased glucagon-like peptide-1 and peptide YY levels relative to pretreatment values, probably by delaying SGLT1-mediated intestinal glucose absorption [1]. LX4211-treated mice and SGLT1-/- mice also had increased GLP-1 AUC values, decreased glucose-dependent insulinotropic polypeptide (GIP) AUC values, and decreased blood glucose excursions during the 6 hours after a challenge with oral glucose alone [2].

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

    Ensayo clínico
    Peso molecular

    424.94

    Fòrmula

    C21H25ClO5S

    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC(C=CC([C@@H]1O[C@H](SC)[C@@H](O)[C@H](O)[C@H]1O)=C2)=C2CC3=CC=C(OCC)C=C3

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    DMSO : ≥ 100 mg/mL (235.33 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 2.3533 mL 11.7664 mL 23.5327 mL
    5 mM 0.4707 mL 2.3533 mL 4.7065 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.

    • Calculadora de molaridad

    • Calculadora de dilución

    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:

    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.88 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 DMSO 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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.
    Pureza y Documentación

    Purity: 99.94%

    Referencias

    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 2.3533 mL 11.7664 mL 23.5327 mL 58.8318 mL
    5 mM 0.4707 mL 2.3533 mL 4.7065 mL 11.7664 mL
    10 mM 0.2353 mL 1.1766 mL 2.3533 mL 5.8832 mL
    15 mM 0.1569 mL 0.7844 mL 1.5688 mL 3.9221 mL
    20 mM 0.1177 mL 0.5883 mL 1.1766 mL 2.9416 mL
    25 mM 0.0941 mL 0.4707 mL 0.9413 mL 2.3533 mL
    30 mM 0.0784 mL 0.3922 mL 0.7844 mL 1.9611 mL
    40 mM 0.0588 mL 0.2942 mL 0.5883 mL 1.4708 mL
    50 mM 0.0471 mL 0.2353 mL 0.4707 mL 1.1766 mL
    60 mM 0.0392 mL 0.1961 mL 0.3922 mL 0.9805 mL
    80 mM 0.0294 mL 0.1471 mL 0.2942 mL 0.7354 mL
    100 mM 0.0235 mL 0.1177 mL 0.2353 mL 0.5883 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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    Nombre del producto:
    Sotagliflozin
    Cat. No.:
    HY-15516
    Cantidad:
    MCE Japan Authorized Agent: