[CAS NO. 156635-05-1] BIBB515
PRODUCTS SPECIFICATIONS [156635-05-1]
DESCRIPTION [156635-05-1]
Overview
| MDL | MFCD00930515 |
|---|---|
| Molecular Weight | 380.87 |
| Molecular Formula | C22H21ClN2O2 |
| SMILES | O=C(C1=CC=C(C=C1)Cl)N2CC/C(CC2)=C\C3=CC=C(C=C3)C4=NCCO4 |
Summary
BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED 50 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] .
IC50 & 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 [ 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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). |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02266485 | Boehringer Ingelheim |
Healthy
|
July 1998 | Phase 1 |
| NCT02266498 | Boehringer Ingelheim |
Healthy
|
June 1998 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 2.5 mg/mL ( 6.56 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6256 mL | 13.1278 mL | 26.2557 mL |
| 5 mM | 0.5251 mL | 2.6256 mL | 5.2511 mL |
| 10 mM | --- | --- | --- |