| Description | S-8921 is an inhibitor of ileal Na+/bile acid cotransporter. |
| In vitro | S-8921 inhibits the uptake velocity of 60 μM [3H] taurocholate dose-dependently in IBAT-COS cells (IC50 value of S-8921: 66±8 μM) [1]. |
| In vivo | S-8921 treatment for 1 to 2 weeks induces a decrease in serum total cholesterol concentrations, with 0.01% S-8921 (4.0 to 4.6 mg/kg) being almost maximally effective. S-8921(Seven-day) treatment induces a dramatic decrease in 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][2]. |
| molecular weight | 540.6 |
| Molecular formula | C30H36O9 |
| CAS | 151165-96-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| 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. 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. |