Shopping Cart

Your shopping cart is currently empty

Lomitapide

Name: Lomitapide
Brand: TargetMol
SKU: T6267
Price: 59 USD
Availability: InStock
Rating: 5 (10 reviews)

😃Good

Catalog No. T6267Cas No. 182431-12-5

Alias BMS-201038, AEGR-733

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.

Lomitapide

😃Good

Purity: 99.40%

Catalog No. T6267Alias BMS-201038, AEGR-733Cas No. 182431-12-5

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$59	In Stock	In Stock
5 mg	$96	In Stock	In Stock
10 mg	$148	In Stock	In Stock
25 mg	$243	In Stock	In Stock
50 mg	$349	In Stock	In Stock
100 mg	$525	In Stock	In Stock
200 mg	$754	In Stock	In Stock
500 mg	$1,160	-	In Stock
1 mL x 10 mM (in DMSO)	$164	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:99.40%

Appearance:Solid

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

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	BMS-201038, AEGR-733

Chemical Properties

Molecular Weight	693.72
Formula	C₃₉H₃₇F₆N₃O₂
Cas No.	182431-12-5
Smiles	FC(F)(F)CNC(=O)C1(CCCCN2CCC(CC2)NC(=O)c2ccccc2-c2ccc(cc2)C(F)(F)F)c2ccccc2-c2ccccc12
Relative Density.	1.34 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 242 mg/mL (348.84 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 93 mg/mL (134.06 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (7.21 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.4415 mL	7.2075 mL	14.4150 mL	72.0752 mL
5 mM	0.2883 mL	1.4415 mL	2.8830 mL	14.4150 mL
10 mM	0.1442 mL	0.7208 mL	1.4415 mL	7.2075 mL
20 mM	0.0721 mL	0.3604 mL	0.7208 mL	3.6038 mL
50 mM	0.0288 mL	0.1442 mL	0.2883 mL	1.4415 mL
100 mM	0.0144 mL	0.0721 mL	0.1442 mL	0.7208 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc