로미타피드

로미타피드
로미타피드 구조식 이미지
카스 번호:
182431-12-5
한글명:
로미타피드
동의어(한글):
로미타피드
상품명:
Lomitapide
동의어(영문):
AEGR 733;BMS 201038;LoMitapide;BMS 201238;BMS 201038-01;AEGR733, BMS201038;AEGR-733(Lomitapide);CB62485047,loMitapide;Lomitapide (10mM in DMSO);AEGR-733(Lomitapide)free base
CBNumber:
CB62485047
분자식:
C39H37F6N3O2
포뮬러 무게:
693.72
MOL 파일:
182431-12-5.mol
MSDS 파일:
SDS

로미타피드 속성

녹는점
142°C(lit.)
끓는 점
778.2±60.0 °C(Predicted)
밀도
1.34±0.1 g/cm3(Predicted)
저장 조건
2-8°C
용해도
DMSO(약간 용해됨), 메탄올(약간 용해됨)
산도 계수 (pKa)
12.66±0.20(Predicted)
물리적 상태
가루
색상
흰색에서 베이지색

안전

HS 번호 2933.39.4100
유해 물질 데이터 182431-12-5(Hazardous Substances Data)

로미타피드 C화학적 특성, 용도, 생산

개요

Lomitapide was approved by the US FDA in December 2012 for the treatment of patients with familial hypercholesteremia (referred to as HoFH) in conjunction with a low-fat diet andother lipid-lowering treatments. Lomitapide was discovered from a high-through put screen that identified several structurally distinct MTP inhibitors. Combination of key structural features from two structurally distinct HTS hits provided potent MTP inhibitors. Parallel analog synthesis led to lomitapide as an optimized structure. Lomitapide was synthesized via alkylation of 9-fluorenylcarboxylic acid with 1,4-dibromobutane which, after trifluoroethylamide formation, provided a bromide intermediate that was displaced by Boc-4-aminopiperidine. Introduction of the 4'-trifluoromethylbiphenylcarboxamide gave lomitapide, which was found to inhibit MTP with an IC50 of 0.5 nM and to exhibit good cholesterol-lowering efficacy in Sprague–Dawley rats (intravenous and oral ED50~0.2 mg/kg).

용도

Lomitapide has been used as a microsomal triglyceride transfer protein (MTP) inhibitor to study its effects on very-low-density lipoproteins (VLDL) export in mouse hepatocytes.

로미타피드 준비 용품 및 원자재

원자재

준비 용품


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