| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Pactimibe targets acyl-CoA:cholesterol acyltransferase (ACAT), a key enzyme in cholesterol metabolism that catalyzes the esterification of cholesterol to cholesteryl esters. By inhibiting ACAT, Pactimibe reduces the accumulation of cholesteryl esters in macrophages and foam cells, thereby stabilizing atherosclerotic plaques. The compound is also used in cosmetic and skin biology research to investigate cholesterol metabolism and lipid storage.
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| ln Vitro |
Pactimibe (CS-505 free base) has the ability to moderately inhibit ACAT in macrophages produced from monocytes, which in turn prevents foam cell production [2].
In vitro, Pactimibe inhibits ACAT activity, reducing cholesteryl ester formation in macrophages and other cell types. The compound has been characterized for its ability to prevent foam cell formation and atherosclerotic plaque progression. In cosmetic and skin biology research, Pactimibe is used to investigate cholesterol metabolism and lipid storage. |
| ln Vivo |
Pactimibe (CS-505 free base; oral gavage; twice daily; 12 weeks) inhibits ACAT-1 and ACAT-2, which lowers plasma cholesterol but has no effect on collagen-positive regions or macrophages[3].
In vivo, Pactimibe has been shown to stabilize atherosclerotic plaque through macrophage ACAT inhibition in WHHL rabbits. The compound has been evaluated in clinical trials studying the treatment of atherosclerosis and coronary heart disease. These studies have assessed the compound's efficacy in reducing atherosclerotic burden and improving cardiovascular outcomes. |
| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for Pactimibe involve ACAT enzyme activity assays using microsomal fractions from liver or macrophages. ACAT activity is measured by incorporating radiolabeled cholesterol (¹⁴C-oleoyl-CoA) into cholesteryl esters. Pactimibe's inhibition of ACAT is determined by measuring the reduction in cholesteryl ester formation.
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| Cell Assay |
In vitro cell-based assays for Pactimibe use macrophage cell lines (such as THP-1-derived macrophages) or hepatocytes. Cells are treated with Pactimibe in the presence of cholesterol and acyl-CoA substrates. Cholesteryl ester accumulation is measured using radioactive or fluorescent cholesterol uptake assays. The compound's effects on foam cell formation and lipid droplet accumulation are assessed.
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| Animal Protocol |
Animal/Disease Models: 8weeks old male C57BL/6J ApoE−/− mice[3]
Doses: 60 and 200 mg/kg/day Route of Administration: po (oral gavage); twice a day; 12-week Experimental Results: 60 and 200 mg/kg/day mg/kg dose, plasma cholesterol levels were diminished by 39% and 74%, respectively. In vivo animal studies for Pactimibe have been conducted in WHHL rabbits, an animal model of atherosclerosis. Rabbits are treated with Pactimibe orally, and atherosclerotic plaque progression and stabilization are assessed histologically. Clinical trials have also been conducted in patients with atherosclerosis and coronary heart disease to evaluate the compound's efficacy and safety. |
| ADME/Pharmacokinetics |
Pactimibe has a molecular formula of C25H40N2O3 and a molecular weight of approximately 416.60 g/mol. The IUPAC name is 7-[(2,2-dimethyl-1-oxopropyl)amino]-2,3-dihydro-4,6-dimethyl-1-octyl-1H-indole-5-acetic acid. The compound has a UNII of D874R9PZ9T. Pactimibe is a small-molecule ACAT inhibitor that is orally bioavailable.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Pactimibe are not extensively detailed in the available literature. The compound has been evaluated in clinical trials, indicating that safety assessments have been conducted. As an ACAT inhibitor, potential toxicities may relate to effects on cholesterol metabolism and lipid homeostasis, though detailed safety profiles are not reported in the provided sources.
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| References |
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| Additional Infomation |
Pactimibe has been used in trials investigating the treatment of atherosclerosis and coronary heart disease.
Pactimibe (CAS 189198-30-9) is a small-molecule ACAT inhibitor that stabilizes atherosclerotic plaque through macrophage ACAT inhibition. It has been studied in clinical trials for the treatment of atherosclerosis and coronary heart disease. The compound is also used in cosmetic and skin biology research to investigate cholesterol metabolism and lipid storage. |
| Molecular Formula |
C25H40N2O3
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|---|---|
| Molecular Weight |
416.606
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| Exact Mass |
416.304
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| CAS # |
189198-30-9
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| Related CAS # |
Pactimibe sulfate;608510-47-0
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| PubChem CID |
3081927
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| Appearance |
White to off-white solid powder
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| Density |
1.071
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| Boiling Point |
604.4ºC at 760 mmHg
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| Flash Point |
319.3ºC
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| Vapour Pressure |
1.86E-15mmHg at 25°C
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| Index of Refraction |
1.547
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| LogP |
5.776
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
30
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| Complexity |
571
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
TXIIZHHIOHVWJD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H40N2O3/c1-7-8-9-10-11-12-14-27-15-13-19-17(2)20(16-21(28)29)18(3)22(23(19)27)26-24(30)25(4,5)6/h7-16H2,1-6H3,(H,26,30)(H,28,29)
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| Chemical Name |
(7-(2,2-Dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl)acetic acid
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| Synonyms |
CS-505 PactimibeCS 505 CS505.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~480.08 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (12.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4003 mL | 12.0016 mL | 24.0033 mL | |
| 5 mM | 0.4801 mL | 2.4003 mL | 4.8007 mL | |
| 10 mM | 0.2400 mL | 1.2002 mL | 2.4003 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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