Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), an enzyme located in the lumen of the endoplasmic reticulum responsible for absorbing dietary lipids and transferring triglycerides onto apolipoprotein B (apo-B) in the assembly of very-low-density lipoprotein.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 59.00 | |
5 mg | In stock | $ 96.00 | |
10 mg | In stock | $ 148.00 | |
25 mg | In stock | $ 243.00 | |
50 mg | In stock | $ 349.00 | |
100 mg | In stock | $ 525.00 | |
200 mg | In stock | $ 754.00 | |
500 mg | In stock | $ 1,160.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 164.00 |
Description | Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), an enzyme located in the lumen of the endoplasmic reticulum responsible for absorbing dietary lipids and transferring triglycerides onto apolipoprotein B (apo-B) in the assembly of very-low-density lipoprotein. |
Targets&IC50 | MTP:8 nM |
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 through cytochrome P-450 (CYP) isoenzyme 3A4 and interacts with CYP3A4 substrates including atorvastatin and simvastatin[2]. |
In vivo | Lomitapide, either as monotherapy or in combination with other lipid-lowering agents, notably reduces low-density lipoprotein cholesterol (LDL-C) levels by over 50%. However, its use is accompanied by significant gastrointestinal side effects and increased hepatic fat. The 50-mg capsule of lomitapide has a bioavailability of 7.1%, and its mean half-life is approximately 39.7 hours[2]. Administration of a single dose of lomitapide can decrease serum triglycerides by 35% and 47% at dosages of 0.3 and 1 mg/kg, respectively. Moreover, multiple-dose regimens have shown a dose-dependent reduction in triglycerides (71%-87%), nonesterified fatty acids (33%-40%), and LDL-C (26-29%)[3]. |
Synonyms | AEGR-733, BMS-201038 |
Molecular Weight | 693.72 |
Formula | C39H37F6N3O2 |
CAS No. | 182431-12-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (134.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 93 mg/mL (134.3 mM)
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Lomitapide 182431-12-5 Metabolism CETP AEGR 733 BMS 201038 Inhibitor AEGR733 BMS201038 AEGR-733 inhibit BMS-201038 inhibitor