BMS 201038
N-(2,2,2-Trifluoroethyl)-9-(4-[4-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl]butyl)-9H-fluorene-9-carboxamide
CAS: 182431-12-5
Molecular Formula: C39H37F6N3O2
BMS 201038 - Names and Identifiers
| Name | N-(2,2,2-Trifluoroethyl)-9-(4-[4-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl]butyl)-9H-fluorene-9-carboxamide |
| Synonyms | AEGR 733 AEGR-733 AEGR733 AEGR 733 Lomitapide BMS 201038 BMS201038 BMS 201238 BMS 201038 BMS-201038 BMS 201038-01 AEGR-733(Lomitapide) N-(2,2,2-Trifluoroethyl)-9-(4-[4-[4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamido]piperidin-1-yl]butyl)-9H-fluorene-9-carboxamide N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide |
| CAS | 182431-12-5 |
BMS 201038 - Physico-chemical Properties
| Molecular Formula | C39H37F6N3O2 |
| Molar Mass | 693.72 |
| Density | 1.34±0.1 g/cm3(Predicted) |
| Melting Point | 142°C(lit.) |
| Boling Point | 778.2±60.0 °C(Predicted) |
| Solubility | DMSO: ≥ 35 mg/mL |
| Appearance | powder |
| Color | white to beige |
| pKa | 12.66±0.20(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | 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. |
| In vivo study | 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. 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%). |
BMS 201038 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.442 ml | 7.208 ml | 14.415 ml |
| 5 mM | 0.288 ml | 1.442 ml | 2.883 ml |
| 10 mM | 0.144 ml | 0.721 ml | 1.442 ml |
| 5 mM | 0.029 ml | 0.144 ml | 0.288 ml |
Last Update：2024-01-02 23:10:35
BMS 201038 - Reference Information
| biological activity | Lomitapide (AEGR-733, BMS-201038) is a potent microsomal triglyceride transfer protein (MTP) inhibitor for the treatment of familial hypercholesterolemia. |
| Target | Value |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-10 22:29:15
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Product Name: Lomitapide Visit Supplier Webpage Request for quotationCAS: 182431-12-5
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Lomitapide Visit Supplier Webpage Request for quotationCAS: 182431-12-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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