RP-64477
Based on 1 Customer Validation
RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).
For research use only. We do not sell to patients.
- Purity: 99.62%
- CAS No.: 135239-65-5
- Formula: C29H42N2O3S
- Molecular Weight:498.72
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
ACAT[1]
RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). Inhibitory potencies of RP-64477 in vitro in tissue preparations are obtained from a range of species and in human cell cultures. For animal tissues, IC50 values in the range 6 to 283 nM are recorded, with no obvious species/tissue differences apparent. Potent inhibitory activity of RP-64477 is also recorded in human cell lines of hepatic (HepGZ), intestinal (CaCo-2), and monocytic (THP-1) origin with IC50s of 503, 113, and 180 nM, respectively. No inhibitory activity is recorded against rat PCEH or LCAT at test concentrations up to 200 μM and 20 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 135239-65-5
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Appearance Solid
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Molecular Weight 498.72
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Formula C29H42N2O3S
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Color White to off-white
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SMILES
O=C(NCCCC)C1=CC=C(SC)C(NC(C2=CC=C(OCCCCCCCCCC)C=C2)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (200.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
ACAT activity is determined in CaCo-2 cells. Cells cultured in 6-well plates are preincubated for 2 hr in 2 mL of Medium 199 supplemented with 10 mM Hepes, pH 7.4, and cholesterol-rich micelles in the presence or absence of RP-64477 that has been initially prepared in neat DMSO. The final concentration of DMSO in the culture medium is 0.2% v/v. Preincubation medium is then replaced with the same medium containing 50 μM [14C] oleic acid complexed with 17 μM bovine serum albumin (fatty acid-free) and cells incubated for a further 2 hr. RP-64477 or vehicle is present during both incubations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Hypocholesterolaemic activity of RP-64477 is investigated by administering RP-64477 (0.00l% to 0.03% w/w by diet) to rats maintained for 3 days on powdered laboratory diet supplemented with cholesterol/cholic acid. Animals are then killed by asphyxiation in carbon dioxide, and terminal blood samples taken by cardiac puncture into a heparinised syringe for preparation of plasma. Plasma cholesterol concentrations are determined enzymatically using standard assay kits. Hypocholesterolaemic activity of RP-64477 in rabbits is investigated by administering RP-64477 at doses of 1, 3, 10, and 30 mg/kg b.i.d. for 7 days to animals receiving standard laboratory diet supplemented with cholesterol. Blood samples are obtained from the central ear artery on days 0 (predosing), 4, and 7 of the study[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (269 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0051 mL | 10.0257 mL | 20.0513 mL | 50.1283 mL |
| 5 mM | 0.4010 mL | 2.0051 mL | 4.0103 mL | 10.0257 mL | |
| 10 mM | 0.2005 mL | 1.0026 mL | 2.0051 mL | 5.0128 mL | |
| 15 mM | 0.1337 mL | 0.6684 mL | 1.3368 mL | 3.3419 mL | |
| 20 mM | 0.1003 mL | 0.5013 mL | 1.0026 mL | 2.5064 mL | |
| 25 mM | 0.0802 mL | 0.4010 mL | 0.8021 mL | 2.0051 mL | |
| 30 mM | 0.0668 mL | 0.3342 mL | 0.6684 mL | 1.6709 mL | |
| 40 mM | 0.0501 mL | 0.2506 mL | 0.5013 mL | 1.2532 mL | |
| 50 mM | 0.0401 mL | 0.2005 mL | 0.4010 mL | 1.0026 mL | |
| 60 mM | 0.0334 mL | 0.1671 mL | 0.3342 mL | 0.8355 mL | |
| 80 mM | 0.0251 mL | 0.1253 mL | 0.2506 mL | 0.6266 mL | |
| 100 mM | 0.0201 mL | 0.1003 mL | 0.2005 mL | 0.5013 mL |
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