| Identification | Back Directory | [Name]
BMS 201038-04 | [CAS]
202914-84-9 | [Synonyms]
BMS 201038-04
AEGR733 Mesylate
AEGR-733 Mesylate
AEGR 733 Mesylate
BMS201038 Mesylate
BMS-201038 Mesylate
BMS 201038 Mesylate
LoMitapide Mesylate
BMS 201038-04 USP/EP/BP
BMS201038/LoMitapide Mesylate
BMS 201038 methanesulfonic acid salt
Inhibitor,Lomitapide,Lomitapide Mesylate,AEGR-733,inhibit,AEGR 733,BMS-201038,AEGR733,BMS201038,BMS 201038
N-(2,2,2-trifluoroethyl)-9-(4-(4-(4'-(trifluoromethyl)biphenyl-2-ylcarboxamido)piperidin-1-yl)butyl)-9H-fluorene-9-carboxamide methanesulfonate
N-(2,2,2-trifluorethyl)-9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide methanesulfonate
N-(2,2,2-Trifluoroethyl)-9-(4-(4-(4'-(trifluoromethyl)-[1,1'-biphenyl]-2-ylcarboxamido)piperidin-1-yl)butyl)-9H-fluorene-9-carboxamide methanesulfonate[AEGR-733 Mesylate | [Molecular Formula]
C39H37F6N3O2.x(CH4O3S) | [MDL Number]
MFCD19443682 | [MOL File]
202914-84-9.mol | [Molecular Weight]
789.826 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,Room Temperature | [solubility ]
DMSO:100.0(Max Conc. mg/mL);126.61(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);126.61(Max Conc. mM) | [form ]
Solid | [color ]
White to off-white | [CAS DataBase Reference]
202914-84-9 |
| Hazard Information | Back Directory | [Description]
Lomitapide is an orally active microsomal triglyceride transfer
protein (MTP) inhibitor for the treatment of hypercholesterolemia.
The drug was developed by Aegerion
Pharmaceuticals Inc. and licensed to Bristol–Myers Squibb Co.
and the University of Pennsylvania. Lomitapide effectively lowered
LDL–cholesterol, both as a single agent and in combination
with commonly prescribed lipid-lowering therapies. Sold under
the trade name Juxtapid, the drug offers a new treatment option
to patients who cannot tolerate statin therapy or who experience
insufficient LDL–cholesterol reduction with the currently available
therapies, such as patients with homozygous familial hypercholesterolemia
caused by mutations in the LDLR gene. | [Uses]
Lomitapide mesylate(AEGR-733; BMS-201038) is an inhibitor of microsomal triglyceride-transfer protein (MTP) wtih in vitro IC50 of 8 nM.
IC50 value: 8 nM [1]
Target: MTP inhibitor
Lomitapide is a small-molecule, microsomal triglyceride transfer protein (MTP) inhibitor, for the treatment of both familial and primary hypercholesterolemia. Oral, once-daily lomitapide will be targeted at patients resistant to HMG-CoA reductase inhibitors (statins) either due to abnormalities in liver function or to discontinuation because of muscle pain. | [Definition]
ChEBI: A methanesulfonate (mesylate) salt prepared from equimolar amounts of lomitapide and methanesulfonic acid. Used as a complement to a low-fat diet and other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia. | [Synthesis]
Commercial 9H-fluorene-9-carboxylic acid (105) was alkylated
with 1,4-dibromobutane in the presence of n-butyl lithium in
THF to give 9-(4-bromobutyl)-9H-fluorene-9-carboxylic acid
(106) in 85% yield. Next, activation of the acid as the acid chloride
followed by coupling with (2,2,2-trifluoroethylamine) provided
amide 107 in 71% yield for the two-step sequence. Displacement
of the terminal bromide with the appropriate 4-carbamoyl
piperidine followed by removal of the Boc group furnished piperidinyl
fluorine 108 in high yield. Amine 108 was then reacted with
the acid chloride derived from acid 109 (derived from the Suzuki
coupling of boronic acid 110 and o-iodobenzoic acid 111) to give
lomitapide, and this was followed by salt formation with methanesulfonic
acid to afford lomitapide mesylate (XIV).
| [storage]
Store at -20°C | [References]
[1] Sulsky R, et al. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70. DOI:10.1016/j.bmcl.2004.07.069
[2] Lomitapide. Am J Cardiovasc Drugs. 2011 Oct 1;11(5):347-52. DOI:10.2165/11533560-000000000-00000
[3] Perry CM. Lomitapide: a review of its use in adults with homozygous familial hypercholesterolemia. Am J Cardiovasc Drugs. 2013 Aug;13(4):285-96. DOI:10.1007/s40256-013-0030-7 |
|
| Company Name: |
Lynnchem
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| Telephone: |
86-(0)29-85992781 17792393971 |
| Website: |
http://www.lynnchem.com/ |
| Company Name: |
Twochem Co.Ltd.
|
| Telephone: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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