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BIBB 515 

Cat. No.: HY-116175 Purity: >99.0%
Handling Instructions

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).

For research use only. We do not sell to patients.

BIBB 515 Chemical Structure

BIBB 515 Chemical Structure

CAS No. : 156635-05-1

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10 mM * 1 mL in DMSO USD 126 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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 [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).
Molecular Weight

380.87

Formula

C₂₂H₂₁ClN₂O₂

CAS No.

156635-05-1

SMILES

O=C(C1=CC=C(C=C1)Cl)N2CC/C(CC2)=C\C3=CC=C(C=C3)C4=NCCO4

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
References

Purity: >99.0%

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Keywords:

BIBB 515BIBB515BIBB-515Others2,3-oxidosqualenecyclaseOSCsterolcholesterolmetabolismlipid-loweringeffectLDLInhibitorinhibitorinhibit

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