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Cat. No.: HY-116719

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BAY 60-5521

BAY 60-5521 is an orally active cholesteryl ester transfer protein (CETP) inhibitor with an IC₅₀ of 7 nM. BAY 60-5521 inhibits CETP-mediated transfer of cholesteryl esters from HDL to LDL/VLDL, as well as the transfer of triglycerides from LDL/VLDL to HDL. It dose-dependently increases HDL-C and HDL concentrations, and slightly reduces triglyceride levels. BAY 60-5521 can be used in studies related to dyslipidemia.

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

CAS No.: 893409-49-9
Formula: C₃₀H₃₇F₄NO
Molecular Weight:503.61

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

BAY 60-5521 Chemical Structure

CAS No.: 893409-49-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
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Biological Activity

Description

In Vitro

BAY 60-5521 (4-18 h) inhibits CETP activity in artificial liposome fluorescence assays, with a mean IC₅₀ of 25 nM, and a mean IC₅₀ of 7 nM measured in human lipoprotein SPA assays^[2].
BAY 60-5521 (24 h) inhibits CETP activity in human plasma and plasma from CETP transgenic mice, with mean IC₅₀ values of 50 nM and 25 nM, respectively^[2].
BAY 60-5521 potently inhibits CETP activity in cell-free CETP fluorescence buffer assays and human plasma, with IC₅₀ values of 0.025 μM and 0.05 μM, respectively^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	AUC	C_max	T_1/2	V_ss	CL	F
Rat^[2]	2 mg/kg	p.o.	1.71 kg·h/L	0.84 L/kg	7.2 h	1.34 L/kg	0.09 L/h/kg	44 %
Dog^[2]	3 mg/kg	p.o.	3.15 kg·h/L	0.70 L/kg	8.60 h	0.56 L/kg	0.50 L/h/kg	74 %

In Vivo

BAY 60-5521 inhibits CETP and increases serum HDL levels in transgenic hCETP mice^[1].
BAY 60-5521 (0.5-2 mg/kg; p.o.; single administration; 16 h-3 days) exerts CETP inhibitory activity and increases HDL-C levels in male CETP transgenic mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CETP transgenic mice (male, 18-25 g, transgenic expression of human CETP)^[2]
Dosage:

0.5 mg/kg; 1 mg/kg; 2 mg/kg (single dose); 2 mg/kg (daily for 3 days)
Administration:

p.o.; single dose for 16 h and 24 h/once daily for 3 days
Result:

Significantly inhibited CETP activity at 16 h and 24 h post-administration with a single oral 2 mg/kg dose.
Increased HDL levels by 53.7% compared to baseline with daily oral 2 mg/kg for 3 days.

Chemical Information

CAS No. 893409-49-9
Molecular Weight 503.61
Formula C₃₀H₃₇F₄NO
SMILES

F[C@@H](C1=CC=C(C=C1)C(F)(F)F)C2=C(C3CCCC3)N=C(CC(C)(C[C@@H]4O)C)C4=C2C5CCCCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Boettcher MF, et al. Single dose pharmacokinetics, pharmacodynamics, tolerability and safety of BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein. British journal of clinical pharmacology. 2012 Feb;73(2):210-8.

[2]. Weber O, et al. Prediction of a potentially effective dose in humans for BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein (CETP) by allometric species scaling and combined pharmacodynamic and physiologically-based pharmacokinetic modelling. British journal of clinical pharmacology. 2012 Feb;73(2):219-31.

[3]. Mantlo NB, et al. Update on the discovery and development of cholesteryl ester transfer protein inhibitors for reducing residual cardiovascular risk. Journal of medicinal chemistry. 2014 Jan 09;57(1):1-17.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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