156635-05-1
156635-05-1 structure
- Name: BIBB 515
- Chemical Name: (4-chlorophenyl)-[4-[[4-(4,5-dihydro-1,3-oxazol-2-yl)phenyl]methylidene]piperidin-1-yl]methanone
- CAS Number: 156635-05-1
- Molecular Formula: C22H21ClN2O2
- Molecular Weight: 380.86700
- Catalog: Research Areas Metabolic Disease
- Create Date: 2016-09-21 07:33:20
- Modify Date: 2025-08-23 15:04:12
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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].
| Name | (4-chlorophenyl)-[4-[[4-(4,5-dihydro-1,3-oxazol-2-yl)phenyl]methylidene]piperidin-1-yl]methanone |
|---|---|
| Synonyms |
(4-Chloro-phenyl)-{4-[4-(4,5-dihydro-oxazol-2-yl)-benzylidene]-piperidin-1-yl}-methanone
BIBB 515 |
| Description | 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]. |
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| Related Catalog | |
| Target |
2,3-oxidosqualene cyclase (OSC)[1] |
| In Vitro | 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: 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 |
| Molecular Formula | C22H21ClN2O2 |
|---|---|
| Molecular Weight | 380.86700 |
| Exact Mass | 380.12900 |
| PSA | 41.90000 |
| LogP | 3.80990 |
| Hazard Codes | Xi |
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