182431-12-5 Usage
Description
N-(2,2,2-Trifluoroethyl)-9-(4-[4-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl]butyl)-9H-fluorene-9-carboxamide, also known as Lomitapide, is a potent microsomal triglyceride transfer protein (MTP) inhibitor. It was developed through a high-throughput screening process and optimized by combining key structural features from two distinct hits. Lomitapide exhibits strong cholesterol-lowering efficacy and has been approved by the US FDA for the treatment of patients with familial hypercholesterolemia (HoFH).
Uses
Used in Pharmaceutical Industry:
Lomitapide is used as a microsomal triglyceride transfer protein (MTP) inhibitor for the treatment of patients with familial hypercholesterolemia (HoFH). It works in conjunction with a low-fat diet and other lipid-lowering treatments to effectively lower cholesterol levels. Lomitapide inhibits MTP with an IC50 of 0.5 nM and demonstrates good cholesterol-lowering efficacy in Sprague–Dawley rats (intravenous and oral ED50~0.2 mg/kg).
Brand name: Juxtapid
Originator
Bristol-Myers Squibb (United States)
Biochem/physiol Actions
Lomitapide is an inhibitor of microsomal triglyceride transfer protein (MTP). Lomitapide has been shown to be highly effective in reducing LDL-cholesterol and triglycerides, and has been aproved for treatment of homozygous familial hypercholesterolemia.
Check Digit Verification of cas no
The CAS Registry Mumber 182431-12-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,8,2,4,3 and 1 respectively; the second part has 2 digits, 1 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 182431-12:
(8*1)+(7*8)+(6*2)+(5*4)+(4*3)+(3*1)+(2*1)+(1*2)=115
115 % 10 = 5
So 182431-12-5 is a valid CAS Registry Number.
182431-12-5Relevant articles and documents
CRYSTALLINE POLYMORPH OF N-(2,2,2-TRIFLUOROETHYL-9-[4-[R4-R[[[I4'- (TRIFLUOROMETHYL) [ 1,1 ' -BIPHENYL] -2-YL] CARBONYL] AMINO] -1 -PIPERIDINYL] BUTYL] -9H- FLUORENE-9-CARBOXAMIDE METHANESULFONATE AND PROCESS FOR PREPARATION THEREOF
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, (2017/07/06)
The present invention relates to? crystalline polymorph of N-(2,2.2-trifluoroethyl)-9- [4- [4- [ [[4,-(trifluoromethyl) [1,1 '-biphenyl] -2-yl] carbonyl] amino] - 1 -piperidinyl] butyl] -9H- fluorene-9-carboxamide methanesulfonate salt represented by the following structural formula- la and process for preparation thereof.
PROCESS FOR THE PREPARATION OF LOMITAPIDE
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, (2016/06/01)
The present invention relates to a process for preparing Lomitapide or its pharmaceutically acceptable salt thereof having high purity with acceptable levels of impurities.
Crystal form III of lomitapide mesylate
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Paragraph 0045; 0046; 0047, (2016/12/01)
The invention provides a crystal form III of lomitapide mesylate. An X-ray diffraction pattern of the crystal form comprises diffraction peaks obtained when a diffraction angle 2theta is equal to 9.912 degrees, 11.584 degrees, 14.651 degrees, 15.444 degre