| Bioactivity | 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]. | |||||||||
| Target | 2,3-oxidosqualene cyclase (OSC) | |||||||||
| Invitro | 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 [14C]-acetate incorporation into digitonin precipitable sterols could be demonstrated in HepG2 cells (ED50 = 4.11 nM). A similar inhibition of OSC activity (ED50= 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[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: | |||||||||
| Name | BIBB 515 | |||||||||
| CAS | 156635-05-1 | |||||||||
| Formula | C22H21ClN2O2 | |||||||||
| Molar Mass | 380.87 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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. |
BIBB 515
CAS: 156635-05-1 F: C22H21ClN2O2 W: 380.87
BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5
Data collection：peptidedb@qq.com
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