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.
Method for synthesizing triglyceride transfer protease inhibitor
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Paragraph 0047; 0048, (2016/12/26)
The invention discloses a method for synthesizing the triglyceride transfer protease inhibitor Lomitapide. Specifically, based on improvement of an existing technique, the compounds 9-carboxyfluorene and 1,4-dibromobutane are used as raw materials, five-step reaction is conducted, and the defects of the prior art are overcome. Compared with the prior art, the method has the main advantage that column chromatography purification is avoided, and product purification is conducted with a recrystallization method which is economical and environment-friendly.
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
