S-8921 |
| رقم الكتالوجGC31541 |
S-8921 هو مثبط ناقل مشتق ileal Na + / حمض الصفراء (IBAT)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 151165-96-7
Sample solution is provided at 25 µL, 10mM.
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S-8921 is an ileal Na+/bile acid cotransporter (IBAT) inhibitor.
S-8921 is an ileal Na+/bile acid cotransporter (IBAT) inhibitor. S-8921 inhibits the uptake velocity of 60 μM [3H] taurocholate dose-dependently in IBAT-COS cells, and the IC50 value of S-8921 is 66±8 μM[1].
Seven-day treatment with S-8921 causes a dramatic decrease of serum cholesterol concentrations in hamsters. The hypocholesterolemic effects of S-8921 are dose-dependent, but S-8921 does not affect body weight. An increase of fecal bile acid excretion is observed especially at higher doses of S-8921[1]. S-8921 treatment for 1 to 2 weeks causes a decrease in serum total cholesterol concentrations, with 0.01% S-8921 (4.0 to 4.6 mg/kg) being almost maximally effective[2].
[1]. Hara S, et al. S-8921, an ileal Na+/bile acid cotransporter inhibitor decreases serum cholesterol in hamsters. Life Sci. 1997;60(24):PL 365-70. [2]. Higaki J, et al. Inhibition of ileal Na+/bile acid cotransporter by S-8921 reduces serum cholesterol and prevents atherosclerosis in rabbits. Arterioscler Thromb Vasc Biol. 1998 Aug;18(8):1304-11.
Cell experiment: | Tripsinized IBAT-COS cells are suspended in the culture medium at the density of 0.8 to 1×105 cells/mL. Aliquots (1 mL) of this suspension are dispersed onto 4-well plastic dishes and the cells are cultured for 48 hours. S-8921 is pre-incubated with the cells for 1 minute when its inhibitory effects are investigated. S-8921 is added as a DMSO solution, with the final concentration of DMSO in buffer A being 0.2 %[1]. |
Animal experiment: | Male golden Syrian hamsters (8 weeks old) are used and given standard powdered diet before starting the experiment and have free access to food and water. The hamsters are divided into six groups so that each group has a similar baseline serum cholesterol concentration. After one more week of adaptation, the animals are either continued on the control diet or switched to a diet supplemented with S-8921 at concentrations of 0.001, 0.003, 0.01, 0.03, and 0.1 % (corresponding to 0.8, 2, 8, 22, and 77 mg/kg/day, respectively) for 7 days. Feces are collected over the last 2 days of the study and lyophylized. The animals are fasted overnight and blood samples are collected from the abdominal aorta under pentobarbital anaesthesia[1]. |
References: [1]. Hara S, et al. S-8921, an ileal Na+/bile acid cotransporter inhibitor decreases serum cholesterol in hamsters. Life Sci. 1997;60(24):PL 365-70. | |
| Cas No. | 151165-96-7 | SDF | |
| Canonical SMILES | O=C(C1=C(C(CC(CC)CC)=O)C(O)=C2C=C(OC)C(OC)=C(OC)C2=C1C3=CC=C(OC)C(OC)=C3)OC | ||
| Formula | C30H36O9 | M.Wt | 540.6 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8498 mL | 9.249 mL | 18.498 mL |
| 5 mM | 370 μL | 1.8498 mL | 3.6996 mL |
| 10 mM | 185 μL | 924.9 μL | 1.8498 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
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