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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

🥰Excellent
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 SizePriceAvailabilityQuantity
1 mg$61In Stock
5 mg$147In Stock
10 mg$237In Stock
25 mg$428In Stock
50 mg$643In Stock
100 mg$965In Stock
1 mL x 10 mM (in DMSO)$175In Stock
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Purity:99.22%
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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.
AliasRP64477
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.
Solubility Information
DMSO: 8.33 mg/mL (16.70 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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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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