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RP-64477

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Catalog No. T8314Cas No. 135239-65-5
Alias RP64477

RP-64477 is the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor.

RP-64477

RP-64477

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Purity: 99.22%
Catalog No. T8314Alias RP64477Cas No. 135239-65-5
RP-64477 is the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$61In StockIn Stock
5 mg$147In StockIn Stock
10 mg$237In StockIn Stock
25 mg$428In StockIn Stock
50 mg$643In StockIn Stock
100 mg$965In StockIn Stock
1 mL x 10 mM (in DMSO)$175In StockIn Stock
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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.
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Purity:99.22%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
RP-64477 is the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor.
In vivo
Inhibition by RP 64477 in a rabbit intestinal enzyme preparation was shown to be non-competitive with respect to the substrate oleoyl-CoA. In whole cell assays using human intestinal (CaCo-2), hepatic HepG2) and monocytic (THP-1) cell lines, RP 64477 inhibited ACAT activity with IC50s of 113, 503, and 180 nM, respectively. RP 64477 (0.03% w/w by diet) reduced significantly cholesterol absorption in cholesterol/cholic acid-fed rats from 94+/- 8% to 65 +/- 4%. In cholesterol-fed rabbits, cholesterol absorption was reduced from 72 +/- 5% to 50 +/-5% and 44 +/- 5% at dose levels of 10 and 30 mg kg-1 b.i.d., respectively. Plasma cholesterol levels were reduced dose-dependently in both cholesterol/cholic-acid-fed rats and cholesterol-fed rabbits. Neither cholesterol absorption nor plasma cholesterol levels were reduced significantly in animals maintained on standard laboratory diets. Pharmacokinetic studies indicated that RP 64477 were very poorly absorbed following oral administration to rats.
SynonymsRP64477
Chemical Properties
Molecular Weight498.72
FormulaC29H42N2O3S
Cas No.135239-65-5
SmilesCCCCCCCCCCOc1ccc(cc1)C(=O)Nc1cc(ccc1SC)C(=O)NCCCC
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 8.33 mg/mL (16.7 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0051 mL10.0257 mL20.0513 mL100.2567 mL
5 mM0.4010 mL2.0051 mL4.0103 mL20.0513 mL
10 mM0.2005 mL1.0026 mL2.0051 mL10.0257 mL

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

Keywords

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