BIBB 515
BIBB 515
CAS: 156635-05-1
Molecular Formula: C22H21ClN2O2
BIBB 515 - Names and Identifiers
BIBB 515 - Physico-chemical Properties
| Molecular Formula | C22H21ClN2O2 |
| Molar Mass | 380.87 |
| Density | 1.26±0.1 g/cm3(Predicted) |
| Boling Point | 586.5±50.0 °C(Predicted) |
| Appearance | White solid. |
| pKa | 4.72±0.50(Predicted) |
| Storage Condition | -20°C，干燥，密封 |
| In vitro study | Sterol synthesis, 2,3-oxidosqualene cyclase activity, HMGCoA reductase activity, and the specificity of BIBB 51 5 versus 2,3-oxidosqualene cyclase are measured in intact HepG2 cells or cell homogenates.Concentration-dependent inhibition of cholesterol biosynthesis by BIBB 515 as monitored by [ 14 C]-acetate incorporation into digitonin precipitable sterols could be demonstrated in HepG2 cells (ED 50 = 4.11 nM). A similar inhibition of OSC activity (ED 50 = 8.69 nM) is seen in HepC2 cell homogenates. No inhibition of HMGCoA reductasc could be measured in HepG2 cell homogenates at concentrations of BIBB 515 up to 1 and 10 μM. |
BIBB 515 - Reference Information
| biological activity | BIBB 515 is a potent, selective and orally active 2, the ED50 values for 3-oxosalene cyclase (OSC) inhibitors are 0.2-0.5 mg/kg and 0.36-33.3 mg/kg (1-5 hours) in rats and mice, respectively. BIBB 515 exerts its lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL). |
| Target | 2,3-oxidosqualene cyclass (OSC) |
| Animal Model: | Male golden Syrian hyperlipemic hamsters (~100 g) |
| Dosage: | 16.0 mg/ kg, 49.7 mg/ kg, and 148.2 mg/ kg |
| Administration: | Oral administration; daily; for 40 days |
| Result: | Dose-dependent lipid-lowering activity was seen in normolipemic hamsters after 11 days treatment (-19% for total cholesterol and -32% for VLDL + LDL cholesterol at 55 mg/kg/day) and in hyperlipemic hamsters after 25 days (-25% for total cholesterol and -59% for LDL-cholesterol at 148 mg/kg/day). |
Last Update：2024-04-10 22:29:15
