1. Membrane Transporter/Ion Channel
  2. Apical Sodium-Dependent Bile Acid Transporter
  3. S-8921

S-8921 是一种回肠 Na+/胆汁酸协同转运蛋白 (IBAT) 的抑制剂。

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S-8921 Chemical Structure

S-8921 Chemical Structure

CAS No. : 151165-96-7

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

S-8921 is an ileal Na+/bile acid cotransporter (IBAT) inhibitor.

IC50 & Target

IBAT[1]

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

540.60

Formula

C30H36O9

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
S-8921
目录号:
HY-19298
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