An internal standard for the quantification of lomitapide
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Unlabeled Version(s)
10009610Lomitapide
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Lomitapide-d8

Item No. 28764

Technical Information
Formal Name
N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl-d8]-9H-fluorene-9-carboxamide
CAS Number
2459377-96-7
Molecular Formula
C39H29D8F6N3O2
Formula Weight
Purity
≥99% deuterated forms (d1-d8)
Formulation
A crystalline solid
Acetonitrile: soluble
SMILES
O=C(NCC(F)(F)F)C1(C([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])N2CCC(NC(C3=CC=CC=C3C4=CC=C(C(F)(F)F)C=C4)=O)CC2)C5=C(C=CC=C5)C6=C1C=CC=C6
InChi Code
InChI=1S/C39H37F6N3O2/c40-38(41,42)25-46-36(50)37(33-13-5-3-10-30(33)31-11-4-6-14-34(31)37)21-7-8-22-48-23-19-28(20-24-48)47-35(49)32-12-2-1-9-29(32)26-15-17-27(18-16-26)39(43,44)45/h1-6,9-18,28H,7-8,19-25H2,(H,46,50)(H,47,49)/i7D2,8D2,21D2,22D2
InChi Key
MBBCVAKAJPKAKM-WKAGHQRMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Lomitapide-d8 is intended for use as an internal standard for the quantification of lomitapide (Item No. 10009610) by GC- or LC-MS. Lomitapide is an inhibitor of microsomal triglyceride transfer protein (MTTP; IC50 = 0.5 nM in a triglyceride transfer assay).1 It inhibits apolipoprotein B (ApoB) secretion in HepG2 cells (EC50 = 0.8 nM). Lomitapide inhibits triglyceride secretion in fasted rats (ED50 = 0.19 mg/kg, p.o.) and reduces total plasma cholesterol levels in hamsters (ED50 = 2.4 mg/kg). It also decreases plasma cholesterol and triglyceride levels in the Watanabe-heritable hyperlipidemic (WHHL) rabbit model of homozygous familial hypercholesterolemia when administered at a dose of 10 mg/kg. Formulations containing lomitapide have been used as an adjunct to a low-fat diet and other lipid-lowering treatments in the treatment of homozygous familial hypercholesterolemia.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wetterau, J.R., Gregg, R.E., Harrity, T.W., et alAn MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits. Science 282(5389), 751-754 (1998).