BIBB 515
BIBB 515 Basic information
- Product Name:
- BIBB 515
- Synonyms:
-
- BIBB 515
- (4-chlorophenyl)-[4-[[4-(4,5-dihydro-1,3-oxazol-2-yl)phenyl]methylidene]piperidin-1-yl]methanone
- Methanone, (4-chlorophenyl)[4-[[4-(4,5-dihydro-2-oxazolyl)phenyl]methylene]-1-piperidinyl]-
- BIBB 515,Inhibitor,OSC,inhibit,cyclase,effect,metabolism,LDL,BIBB-515,2,3-oxidosqualene,BIBB515,sterol,cholesterol,lipid-lowering
- BIBB 515, 10 mM in DMSO
- CAS:
- 156635-05-1
- MF:
- C22H21ClN2O2
- MW:
- 380.87
- Mol File:
- 156635-05-1.mol
BIBB 515 Chemical Properties
- Boiling point:
- 586.5±50.0 °C(Predicted)
- Density
- 1.26±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:1.38(Max Conc. mg/mL);3.62(Max Conc. mM)
DMF:0.3(Max Conc. mg/mL);0.79(Max Conc. mM)
Ethanol:0.15(Max Conc. mg/mL);0.39(Max Conc. mM) - form
- White solid.
- pka
- 4.72±0.50(Predicted)
- color
- White to off-white
BIBB 515 Usage And Synthesis
Uses
BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL)[1].
in vivo
BIBB 515 (16.0-148.2 mg/ kg; oral administration; daily; for 40 days; male golden Syrian hyperlipemic hamsters) treatment shows dose-dependent lipid-lowering activity in normolipemic hamsters (-19% for total cholesterol and -32% for VLDL + LDL cholesterol) and in hyperlipemic hamsters (-25% for total cholesterol and -59% for LDL-cholesterol)[1].
| Animal Model: | Male golden Syrian hyperlipemic hamsters (~100 g)[1] |
| 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). |
References
[1] Eisele B, et al. Effects of a novel 2,3-oxidosqualene cyclase inhibitor on cholesterol biosynthesis and lipid metabolism in vivo. J Lipid Res. 1997 Mar;38(3):564-75. PMID:9101437
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