2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Autophagy Apoptosis
  3. Microsomal Triglyceride Transfer Protein (MTP) mTOR LDLR Autophagy Apoptosis
  4. Lomitapide mesylate

Lomitapide mesylate  (Synonyms: AEGR-733 mesylate; BMS-201038 mesylate)

Cat. No.: HY-14668 Purity: 99.57%
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Lomitapide (AEGR-733; BMS-201038) mesylate is an orally active microsomal triglyceride transfer protein (MTP) inhibitor and a selective mTORC1 inhibitor with lipid-lowering activity and BBB permeability. Lomitapide mesylate significantly reduces plasma LDL levels by blocking the assembly and secretion of very-low-density lipoprotein (VLDL). Lomitapide mesylate inhibits mTORC1 in an ATP-dependent manner, thereby inducing AMPK-independent autophagic cell death and suppressing cancer cell growth and apoptosis. Lomitapide mesylate also enhances tumor infiltration of CD8+ T cells. In addition, Lomitapide mesylate inhibits HDAC, improves endothelial function, effectively alleviates vascular inflammation and oxidative stress, and exerts neuroprotective effects in a cerebral ischemia/reperfusion injury model. Lomitapide mesylate can be used in research on related diseases such as colorectal cancer, breast cancer, melanoma, ischemic stroke, and familial hypercholesterolemia.

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

CAS No. : 202914-84-9

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10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 6 publication(s) in Google Scholar

Other Forms of Lomitapide mesylate:

Lomitapide mesylate Related Antibodies

Top Publications Citing Use of Products

    Lomitapide mesylate purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Jun;36(24):e2311760.  [Abstract]

    Lomitapide (LMP) (10 μM; 21 d) significantly inhibited the growth of 3D U251 cells.

    Lomitapide mesylate purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Jun;36(24):e2311760.  [Abstract]

    Lomitapide (LMP) (5.8 μM) induced apoptosis in GBM cells.

    Lomitapide mesylate purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Jun;36(24):e2311760.  [Abstract]

    Lomitapide (LMP) (2.5-10 μM; 24 h) exhibited a concentration-dependent increase in cytotoxicity against U118 cells.

    Lomitapide mesylate purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Jun;36(24):e2311760.  [Abstract]

    Lomitapide (LMP) (5.8 μM) mainly induced GBM cells to undergo early apoptosis.

    Lomitapide mesylate purchased from MedChemExpress. Usage Cited in: Adv Mater. 2024 Jun;36(24):e2311760.  [Abstract]

    Lomitapide (LMP) (5.8 μM) induced the oligomeric GSDMD-N-terminal structural domains to aggregate on the membrane, thereby expediting pyroptosis of U251 cells.

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    Description

    Lomitapide (AEGR-733; BMS-201038) mesylate is an orally active microsomal triglyceride transfer protein (MTP) inhibitor and a selective mTORC1 inhibitor with lipid-lowering activity and BBB permeability. Lomitapide mesylate significantly reduces plasma LDL levels by blocking the assembly and secretion of very-low-density lipoprotein (VLDL). Lomitapide mesylate inhibits mTORC1 in an ATP-dependent manner, thereby inducing AMPK-independent autophagic cell death and suppressing cancer cell growth and apoptosis. Lomitapide mesylate also enhances tumor infiltration of CD8+ T cells. In addition, Lomitapide mesylate inhibits HDAC, improves endothelial function, effectively alleviates vascular inflammation and oxidative stress, and exerts neuroprotective effects in a cerebral ischemia/reperfusion injury model. Lomitapide mesylate can be used in research on related diseases such as colorectal cancer, breast cancer, melanoma, ischemic stroke, and familial hypercholesterolemia[1][2][3][4].

    Cellular Effect
    Cell Line Type Value Description References
    HepG2 ED50
    0.8 nM
    Compound: Juxtapid
    Inhibition of ApoB lipoprotein secretion in human HepG2 cells
    Inhibition of ApoB lipoprotein secretion in human HepG2 cells
    		[PMID: 38889609]
    In Vitro

    Lomitapide mesylate (5 μM; 48 h) inhibits the proliferation of human HCT116, HT29 and SW480 colorectal cancer cells by reducing colony formation, and (2 μM; 96 h) inhibits the proliferation of HT29 cells overexpressing eIF4E[1].
    Lomitapide mesylate (5 μM; 24 h) induces autophagic cell death in human HCT116 and HT29 colorectal cancer cells; autophagy inhibition restores cell viability, while no apoptosis-related caspase 3/7 activity is detected[1].
    Lomitapide mesylate (5-20 μM; 48-72 h) potently inhibits the growth and induces autophagy in patient-derived human colorectal cancer organoids CRC-01 and CRC-02, and exhibits better efficacy than 5-FU (HY-90006) at equivalent concentrations[1].
    Lomitapide mesylate (0.01-1 μM; 24 h) shows no toxicity to mouse Neuro-2a cells, and improves the survival rate of OGD-injured Neuro-2a cells in a concentration-dependent manner[2].
    Lomitapide mesylate (0.01-1 μM; 24 h) shows no toxicity to primary mouse cortical neurons, and improves the cell viability of primary mouse cortical neurons injured by OGD in a concentration-dependent manner[2].
    Lomitapide mesylate restores autophagic flux and inhibits apoptosis in OGD-injured mouse Neuro-2a cells co-cultured with LPS-treated BV2 microglia, which is evidenced by the normalization of autophagy protein expression and increased Bcl-2 levels[2].
    Lomitapide mesylate significantly inhibits the migration of mouse BV2 microglial cells toward OGD-injured Neuro-2a cells[2].

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

    Lomitapide mesylate Related Antibodies

    Western Blot Analysis[1]

    Cell Line: HEK293T cells
    Concentration: 10-100 μM; 50 μM with 500-5000 μM ATP
    Incubation Time: 15 min at 37 °C
    Result: Dose-dependently inhibited phosphorylation of the mTORC1 substrate T389 S6K1, with reduced phosphorylation observed at all tested concentrations.
    Showed reversed inhibitory effect when ATP concentrations were increased, indicating competition with ATP for binding to mTORC1.
    Exhibited no inhibition of mTORC2 activity (measured by S473 Akt phosphorylation).

    Cell Autophagy Assay[1]

    Cell Line: Human colorectal cancer cell lines (HCT116, HT29)
    Concentration: 5 μM; 5 μM with 1 mM 3-MA; 5 μM with bafilomycin
    Incubation Time: 24 h
    Result: Increased GFP-LC3 puncta formation in HT29 cells, indicating autophagosome accumulation.
    Showed rescued cell viability reduction when treated with bafilomycin (in HT29 cells) or 3-MA (in HCT116 cells).
    Showed inhibited LC3-II elevation when treated with 3-MA, and diminished LC3-II levels when ATG7 or Beclin-1 was knocked down.
    Did not induce caspase 3/7 activity, indicating no apoptotic response.

    Cell Viability Assay[2]

    Cell Line: murine Neuro-2a cells
    Concentration: 0.01, 0.1, 1 μM
    Incubation Time: 24 h; 4 h (OGD exposure prior to treatment)
    Result: Showed no cytotoxicity at all tested concentrations compared to control.
    Alleviated cell damage and improved cell viability in a concentration-dependent manner in OGD-injured cells, with statistically significant differences relative to the OGD model group.
    In Vivo

    Lomitapide (10-50 mg/kg; intraperitoneal injection; once every 2 days for 10 days) mesylate potently inhibits the growth of colorectal cancer xenografts in BALB/c nude mice; at the dose of 20 mg/kg, it reduces the volume of HT29 tumors to approximately 38% of that in the vehicle control group, with no observed toxicity[1].
    Lomitapide (20 mg/kg; intraperitoneal injection; administered 5 times; initiated on day 10 post tumor implantation) mesylate inhibits the growth of MC38 colorectal cancer and B16-F10 melanoma in C57B6/N mice, respectively[1].
    Lomitapide (0.5 mg/kg; p.o.; once daily; for 14 consecutive days) mesylate significantly improves neurological function, reduces neuronal tissue loss by 41.05%, enhances neuronal autophagy, inhibits the migration of pro-inflammatory microglia, and increases the survival rate of mice with ischemic stroke induced by middle cerebral artery occlusion (MCAO)[2].
    Lomitapide (1 mg/kg/day; oral administration; daily dosing; for 2 consecutive weeks) mesylate improves cardiovascular function, reduces body weight and fat mass, downregulates blood glucose and lipid levels, decreases atherosclerotic plaque area, and alleviates vascular stress and inflammatory responses in obese LDLr−/− mice[3].

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

    Animal Model: C57B6/N (6-week-old wild-type female; 6-week-old wild-type male; subcutaneous implantation of MC38 colorectal cancer cells)[1]
    Dosage: 20 mg/kg
    Administration: i.p.; 5 doses; starting 10 days post-tumor injection
    Result: Achieved a tumor growth inhibition (TGI) of 66%.
    Did not cause changes in mouse body weight.
    Showed no toxicity in liver, kidney, or lung tissues.
    Increased infiltration of CD8+ T cells into tumor tissues.
    Animal Model: C57B6/N (6-week-old wild-type female; 6-week-old wild-type male; subcutaneous implantation of B16-F10 melanoma cells)[1]
    Dosage: 20 mg/kg
    Administration: i.p.; 5 doses every other day; starting 10 days post-tumor injection
    Result: Reduced B16-F10 melanoma tumor growth.
    Did not cause changes in mouse body weight.
    Showed no toxicity in liver, kidney, or lung tissues.
    Clinical Trial
    Molecular Weight

    789.83

    Formula

    C40H41F6N3O5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1(CCCCN2CCC(NC(C3=CC=CC=C3C4=CC=C(C(F)(F)F)C=C4)=O)CC2)C5=C(C6=C1C=CC=C6)C=CC=C5)NCC(F)(F)F.O=S(C)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (126.61 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 1.2661 mL 6.3305 mL 12.6610 mL
    5 mM 0.2532 mL 1.2661 mL 2.5322 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

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    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.17 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 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: ≥ 2.5 mg/mL (3.17 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.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 99.61%

    SDS (252 KB)

    COA (252 KB) HNMR (337 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    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 (sealed storage, away from moisture). 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 1 mM 1.2661 mL 6.3305 mL 12.6610 mL 31.6524 mL
    5 mM 0.2532 mL 1.2661 mL 2.5322 mL 6.3305 mL
    10 mM 0.1266 mL 0.6330 mL 1.2661 mL 3.1652 mL
    15 mM 0.0844 mL 0.4220 mL 0.8441 mL 2.1102 mL
    20 mM 0.0633 mL 0.3165 mL 0.6330 mL 1.5826 mL
    25 mM 0.0506 mL 0.2532 mL 0.5064 mL 1.2661 mL
    30 mM 0.0422 mL 0.2110 mL 0.4220 mL 1.0551 mL
    40 mM 0.0317 mL 0.1583 mL 0.3165 mL 0.7913 mL
    50 mM 0.0253 mL 0.1266 mL 0.2532 mL 0.6330 mL
    60 mM 0.0211 mL 0.1055 mL 0.2110 mL 0.5275 mL
    80 mM 0.0158 mL 0.0791 mL 0.1583 mL 0.3957 mL
    100 mM 0.0127 mL 0.0633 mL 0.1266 mL 0.3165 mL
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    Lomitapide mesylate Related Classifications

    Help & FAQs
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      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.

    Keywords:

    Lomitapide202914-84-9AEGR-733BMS-201038AEGR733AEGR 733BMS201038BMS 201038Microsomal Triglyceride Transfer Protein (MTP)mTORLDLRAutophagyApoptosisMammalian target of RapamycinLow-density lipoprotein receptormTORC2LDL receptor-knockout micevery low-density lipoproteinhistone deacetylaselow-density lipoprotein particlehepatic microsomal triglyceride transfer proteincerebral ischemia/reperfusion injury modelsCD8+ T cellmTORC1chylomicronInhibitorinhibitorinhibit

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