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RP-64477 Acyltransferase inhibitor

Cat.No.S0820

RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). This compound inhibits ACAT activity with IC50 of 113 nM, 503 nM, and 180 nM in human intestinal (CaCo-2), hepatic (HepG2) and monocytic (THP-1) cell assays, respectively.
RP-64477 Acyltransferase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 498.72

Quality Control

Batch: S082001 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.69%
99.69

Chemical Information, Storage & Stability

Molecular Weight 498.72 Formula

C29H42N2O3S

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 135239-65-5 -- Storage of Stock Solutions

Synonyms N/A Smiles CCCCCCCCCCOC1=CC=C(C=C1)C(=O)NC2=C(C=CC(=C2)C(=O)NCCCC)SC

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (200.51 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
ACAT [1]
(CaCo-2 cell-based assay)
113 nM
ACAT [1]
(THP-1 cell-based assay)
180 nM
ACAT [1]
(HepG2 cell-based assay)
503 nM
References

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