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Purity: ≥98%
Lomitapide (formerly known as AEGR-733; BMS-201038; Juxtapid; Lojuxta) is a novel, oral and potent inhibitor of microsomal triglyceride-transfer protein (MTP) approved as a lipid-lowering agent for the treatment of homozygous familial hypercholesterolemia. It inhibits MTP with an IC50 of 8 nM in vitro. As an orally active MTP inhibitor, Lomitapide is indicated as an adjunct to a low-fat diet and other lipid-lowering treatments, including LDL apheresis where available for the reduction of LDL-C, total cholesterol, apolipoprotein B, and non-high-density lipoprotein cholesterol in adult patients with HoFH.
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| ln Vitro |
An oral microsomal triglyceride transfer protein (MTP) inhibitor called lipitpide is used to treat patients with homoeopathy of function (HoFH), an uncommon type of hypercholesterolemia that causes early atherosclerotic disease. Cytochrome P-450 (CYP) isoenzyme 3A4 is responsible for the hepatic metabolism of lomitapide. It has an interaction with CYP3A4 substrates, such as Simvastatin and Atorvastatin [2].
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| ln Vivo |
Lomitapide lowers plasma concentrations of low-density lipoprotein cholesterol (LDL-C) by an average of more than 50% when used by itself or in conjunction with other lipid-lowering medications. Significant gastrointestinal side effects and elevated levels of hepatic fat are linked to lomitapide. For 50 mg of lomitapide, the bioavailability is 7.1%. Lomapide has an average half-life of 39.7 hours [2]. It was demonstrated that lomitapide, at doses of 0.3 mg/kg and 1 mg/kg, respectively, reduced serum triglycerides by 35% and 47% after just one treatment. Dose-dependent decreases in triglycerides (71%–87%), nonesterified fatty acids (33%–40%), and low-density lipoprotein cholesterol (26–29%) were also observed after multiple-dose lomitapide treatment [3].
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| 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.
[2]. Davis KA. et al. Lomitapide: A novel agent for the treatment of homozygous familial hypercholesterolemia. Am J Health Syst Pharm. 2014 Jun 15;71(12):1001-8. [3]. Dhote V, et al. 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 |
| Molecular Formula |
C39H37N3O2F6
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|---|---|
| Molecular Weight |
693.72038
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| CAS # |
182431-12-5
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| Related CAS # |
Lomitapide mesylate;202914-84-9;Lomitapide-d8;2459377-96-7
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| SMILES |
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
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| InChi Key |
MBBCVAKAJPKAKM-UHFFFAOYSA-N
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| 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)
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| 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
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| Synonyms |
BMS 201038; AEGR733; BMS-201038; AEGR-733; BMS201038; BMS 201038-01; AEGR 733; Lomitapide mesylate. trade name: Juxtapid; Lojuxta.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~144.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (3.60 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4415 mL | 7.2075 mL | 14.4150 mL | |
| 5 mM | 0.2883 mL | 1.4415 mL | 2.8830 mL | |
| 10 mM | 0.1442 mL | 0.7208 mL | 1.4415 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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