Referencia número: HY-14668

Lomitapide mesylate

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

6 Cited Publications

Revisión del cliente

Based on 6 publication(s) in Google Scholar

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.

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Pureza: 99.57%
No. CAS: 202914-84-9
Fòrmula: C₄₀H₄₁F₆N₃O₅S
Peso molecular:789.83

Almacenamiento:

4°C, sealed storage, away from moisture

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

Lomitapide mesylate Chemical Structure

No. CAS: 202914-84-9

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (6)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Bioz

Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas mTOR :

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.

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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 202914-84-9
Appearance Solid
Peso molecular 789.83
Fòrmula C₄₀H₄₁F₆N₃O₅S
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
Synonyms

AEGR-733 mesylate; BMS-201038 mesylate
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

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

Publications (6)

All Cell Proliferation/Viability AssayCell Imaging/StainingFlow Cytometry

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Journal Impact Factor

Adv Mater

Efficient Delivery of Lomitapide using Hybrid Membrane-Coated Tetrahedral DNA Nanostructures for Glioblastoma Therapy. [Abstract]

2024 Jun;36(24):e2311760. PMID: 38569065

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.
Free Radic Biol Med

Lipid overload impairs hepatic VLDL secretion via oxidative stress-mediated PKCδ-HNF4α-MTP pathway in large yellow croaker (Larimichthys crocea). [Abstract]

2021 Aug 20:172:213-225. PMID: 34116177
Liver Int

Disentangling Organ-Specific Roles of Farnesoid X Receptor in Bile Acid and Glucolipid Metabolism. [Abstract]

2025 Apr;45(4):e70027. PMID: 40052709
BMC Microbiol

Antibacterial activities and action mode of anti-hyperlipidemic lomitapide against Staphylococcus aureus. [Abstract]

2022 Apr 26;22(1):114. PMID: 35473561
J Lipid Res

Therapeutic siRNA targeting PLIN2 ameliorates steatosis, inflammation, and fibrosis in steatotic liver disease models. [Abstract]

2024 Aug 24:100635. PMID: 39187042
bioRxiv

2025 Jul 21.

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2661 mL

6.3305 mL

12.6610 mL

5 mM

0.2532 mL

1.2661 mL

2.5322 mL

10 mM

0.1266 mL

0.6330 mL

1.2661 mL

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (3.17 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (287 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Lee B, et al. Lomitapide, a cholesterol-lowering drug, is an anticancer agent that induces autophagic cell death via inhibiting mTOR. Cell Death Dis. 2022;13(7):603. Published 2022 Jul 12. [Content Brief]

[2]. Zheng Y, et al. Lomitapide ameliorates middle cerebral artery occlusion-induced cerebral ischemia/reperfusion injury by promoting neuronal autophagy and inhibiting microglial migration. CNS Neurosci Ther. 2022;28(12):2183-2194. [Content Brief]

[3]. Munkhsaikhan U, et al. The Beneficial Effect of Lomitapide on the Cardiovascular System in LDLr^-/- Mice with Obesity. Antioxidants (Basel). 2023;12(6):1287. Published 2023 Jun 16. [Content Brief]

[4]. Won JI, et al. Balancing Low-density Lipoprotein Cholesterol Reduction and Hepatotoxicity With Lomitapide Mesylate and Mipomersen in Patients With Homozygous Familial Hypercholesterolemia. Rev Cardiovasc Med. 2017;18(1):21-28. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Lomitapide mesylate

6 Cited Publications

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Lomitapide mesylate

Apoptosis Compound Library

Kinase Inhibitor Library

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Publications Citing Use of MedChemExpress (MCE) Lomitapide mesylate

Ver todos los productos específicos de isoformas mTOR

Actividad biológica

Chemical Information

Publications (6)

Solvente y solubilidad

Pureza y Documentación