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Lomitapide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lomitapide图片
CAS NO:182431-12-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件

Name: Lomitapide free base
CAS#: 182431-12-5 (free base)
Chemical Formula: C39H37F6N3O2
Exact Mass: 693.279
Molecular Weight: 693.73442
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Technical InformationSynonym: BMS 201038; AEGR733; BMS-201038; AEGR-733; BMS201038; BMS 201038-01; AEGR 733; Lomitapide mesylate. trade name: Juxtapid; Lojuxta.
Chemical Name: N-(2,2,2-trifluoroethyl)-9-(4-(4-(4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamido)piperidin-1-yl)butyl)-9H-fluorene-9-carboxamide
InChi Key: MBBCVAKAJPKAKM-UHFFFAOYSA-N
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)
SMILES Code: O=C(NCC(F)(F)F)C1(C2=C(C=CC=C2)C3=C1C=CC=C3)CCCCN4CCC(CC4)NC(C5=CC=CC=C5C6=CC=C(C=C6)C(F)(F)F)=O
实验参考方法
Target

IC50: 8 nM (MTP)[1]

In Vitro Lomitapide is an oral microsomal triglyceride transfer protein (MTP) inhibitor indicated for the treatment of patients with HoFH, a rare form of hypercholesterolemia that can lead to premature atherosclerotic disease. Lomitapide undergoes hepatic metabolism via cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including atorvastatin and simvastatin[2].
In Vivo The use of lomitapide alone or in combination with other lipid-lowering modalities reduces plasma concentrations of low density lipoprotein cholesterol (LDL-C) by a mean of more than 50%. Lomitapide is associated with significant gastrointestinal adverse effects and increases in hepatic fat levels. The bioavailability of the 50-mg lomitapide capsule is 7.1%. The mean half-life of lomitapide is 39.7 hours[2]. Single-dose administration of lomitapide is shown to reduce serum triglycerides by 35% and 47% at 0.3- and 1-mg/kg doses, respectively. Multiple-dose treatment with lomitapide also results in dose dependent decrease in triglycerides (71%–87%), nonesterified fattyacids(33%–40%), and LDL-C(26-29%)[3].
Animal Exp Rats: BMS-201038 is formulated in 0.1% hydroxyl ethyl cellulose and 0.5% Tween 80 in deionized water. Rats in the control group are administered vehicle (2 mL/kg) p.o. Fasted rats are administered 0.3 and 1 mg/kg, p.o., BMS-201038, followed 1 h later by 250 mg/kg, i.v., Triton WR1339. Blood samples are obtained from rats up to 240 min after Triton WR1339 injection to estimate serum triglyceride concentrations. For evaluation of post-prandial lipaemia, fasted rats are administered 0.3 and 1 mg/kg, p.o., BMS-201038, followed 1 h later by a corn oil bolus (6 mL/kg) by oral gavage. Blood samples are again collected up to 1440 min after corn oil administration for the estimation of serum triglyceride concentrations[3].
References

[1]. 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70.

[2]. Lomitapide: A novel agent for the treatment of homozygous familial hypercholesterolemia. Am J Health Syst Pharm. 2014 Jun 15;71(12):1001-8.

[3]. Inhibition of microsomal triglyceride transfer protein improves insulin sensitivity and reduces atherogenic risk in Zucker fatty rats. Clin Exp Pharmacol Physiol. 2011 May;38(5):338-44.