1. Metabolic Enzyme/Protease
  2. Phospholipase
  3. ML348

ML348 (GNF-Pf-1127) is a selective and reversible acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2.

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No. CAS : 899713-86-1

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

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ML348 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 21;14(1):6682.  [Abstract]

    ML348 (4–16 μM, 12–36 h) decreased the abundance of β-catenin (including its active form) and Cyclin D1, and increased its phosphorylated form in PTCs.

    ML348 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 21;14(1):6682.  [Abstract]

    ML348 (intraperitoneal injection 3.2 mg/kg/day, 10 days) markedly attenuated interstitial matrix deposition and tubular atrophy in mice after UUO.

    ML348 purchased from MedChemExpress. Usage Cited in: Adv Mater. 2021 Dec;33(49):e2103471.  [Abstract]

    ML348 (5 μM, 24 h) increased the infection efficiency of the pseudotype virus in ML348-pretreated cells.

    ML348 purchased from MedChemExpress. Usage Cited in: Adv Mater. 2021 Dec;33(49):e2103471.  [Abstract]

    ML348 (5 μM, 24 h) increased the infection efficiency of the pseudotype virus in ML348-pretreated cells.

    ML348 purchased from MedChemExpress. Usage Cited in: Adv Mater. 2021 Dec;33(49):e2103471.  [Abstract]

    ML348 (5 μM, 48 h) increased the infection efficiency of the pseudotype virus in HEK293T cells stably expressing ACE2 upon infection with SARS-CoV-2-GFP pseudovirus (MOI of 1).

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    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    ML348 (GNF-Pf-1127) is a selective and reversible acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2[1].

    IC50 & Target

    IC 50: 210 nM (LYPLA1)

    Cellular Effect
    Cell Line Type Value Description References
    Huh-7 CC50
    >100 μM
    Compound: GNF-Pf-1127
    NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
    NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
    [PMID: 18579783]
    In Vitro

    ML348 (5 μM; 3 hours ) selectively inhibits LYPLA1 in cultured cells[1].

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

    Cell Viability Assay[1]

    Cell Line: HEK293T cells, murine T-cells
    Concentration: 5 µM
    Incubation Time: 3 hours
    Result: Show potent, selective inhibition of LYPLA1.
    In Vivo

    ML348 (50 mg/kg, i.p., 3 hours) shows potent and selective activity in vivo, inhibits LYPLA1 enzymes in heart, kidney and lung in mice[1].

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

    Animal Model: C57BL6 male mice (3-4 months)[1]
    Dosage: 50 mg/kg
    Administration: Intraperitoneal injection; 3 hours
    Result: Potent and selective inhibited LYPLA1 enzymes in heart, kidney and lung in vivo.
    Peso molecular

    415.79

    Fòrmula

    C18H17ClF3N3O3

    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC(C(F)(F)F)=CC=C1Cl)CN2CCN(C(C3=CC=CO3)=O)CC2

    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 : 25 mg/mL (60.13 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 2.4051 mL 12.0253 mL 24.0506 mL
    5 mM 0.4810 mL 2.4051 mL 4.8101 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.01 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: 99.97%

    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 2.4051 mL 12.0253 mL 24.0506 mL 60.1265 mL
    5 mM 0.4810 mL 2.4051 mL 4.8101 mL 12.0253 mL
    10 mM 0.2405 mL 1.2025 mL 2.4051 mL 6.0127 mL
    15 mM 0.1603 mL 0.8017 mL 1.6034 mL 4.0084 mL
    20 mM 0.1203 mL 0.6013 mL 1.2025 mL 3.0063 mL
    25 mM 0.0962 mL 0.4810 mL 0.9620 mL 2.4051 mL
    30 mM 0.0802 mL 0.4008 mL 0.8017 mL 2.0042 mL
    40 mM 0.0601 mL 0.3006 mL 0.6013 mL 1.5032 mL
    50 mM 0.0481 mL 0.2405 mL 0.4810 mL 1.2025 mL
    60 mM 0.0401 mL 0.2004 mL 0.4008 mL 1.0021 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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    Inquiry Information

    Nombre del producto:
    ML348
    Cat. No.:
    HY-100736
    Cantidad:
    MCE Japan Authorized Agent: