Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
Other Sizes |
|
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].
|
---|---|
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].
|
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. |
References |
|
Additional Infomation |
Pactimibe has been used in trials studying the treatment of Atherosclerosis and Coronary Heart Disease.
|
Molecular Formula |
C25H40N2O3
|
---|---|
Molecular Weight |
416.606
|
Exact Mass |
416.304
|
CAS # |
189198-30-9
|
Related CAS # |
Pactimibe sulfate;608510-47-0
|
PubChem CID |
3081927
|
Appearance |
White to off-white solid powder
|
Density |
1.071
|
Boiling Point |
604.4ºC at 760 mmHg
|
Flash Point |
319.3ºC
|
Vapour Pressure |
1.86E-15mmHg at 25°C
|
Index of Refraction |
1.547
|
LogP |
5.776
|
Hydrogen Bond Donor Count |
2
|
Hydrogen Bond Acceptor Count |
4
|
Rotatable Bond Count |
11
|
Heavy Atom Count |
30
|
Complexity |
571
|
Defined Atom Stereocenter Count |
0
|
InChi Key |
TXIIZHHIOHVWJD-UHFFFAOYSA-N
|
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)
|
Chemical Name |
(7-(2,2-Dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl)acetic acid
|
Synonyms |
CS-505 PactimibeCS 505 CS505.
|
HS Tariff Code |
2934.99.9001
|
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)
|
Solubility (In Vitro) |
DMSO : ~200 mg/mL (~480.08 mM)
|
---|---|
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.