202914-84-9
Chemical Structure
Lomitapide mesylate
Synonym(s): AEGR-733 mesylate; BMS-201038 mesylate
- CAS No.: 202914-84-9
- Formula:C40H41F6N3O5S
- Molecular Weight:789.83
IUPAC Name: N-(2,2,2-trifluoroethyl)-9-(4-(4-(4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamido)piperidin-1-yl)butyl)-9H-fluorene-9-carboxamide methanesulfonate
InChIKey: QKVKOFVWUHNEBX-UHFFFAOYSA-N
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
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Lomitapide mesylate | 99.57% | 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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Lomitapide mesylate (Standard) | ≥98% | Lomitapide (mesylate) (Standard) is the analytical standard of Lomitapide (mesylate). This product is intended for research and analytical applications. Lomitapide (AEGR-733; BMS-201038) mesylate is a highly effective MTP protein inhibitor with an in vitro IC50 value of 8nM. | ||||||||||||||||||||
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- [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]
