Now on opnMe: Order BI-5756, a cholesteryl ester transfer protein (CETP) inhibitor
25 April 2022
Cholesteryl ester transfer protein (CETP) is a glycoprotein that mediates the exchange of cholesteryl ester from high-density lipoprotein (HDL). Transfer of cholesterol from extrahepatic tissues to the liver appears to be the major atheroprotective function of HDL, and an elevation of HDL levels could represent an effective strategy.
However, although several CETP inhibitors have proven their HDL-C-increasing effect as part of preclinical studies, the cardiovascular-protective effects during later stages of development were inconsistent. None of the CETP inhibitors that reached clinical investigation had been able to obtain regulatory approval, thus questioning the suitability of this mode of action in the context of human disease. However, given the recent evidence that the physiological role of HDL-C is more complex than previously thought, there remains an interest to continue studying CETP inhibition. We are glad to share our CETP inhibitor BI-5756 with the scientific community to foster novel approaches.
BI-5756 is a polar CETP inhibitor with reduced lipophilicity and improved solubility compared to other CETP inhibitors. It has a comparatively fast elimination from fat tissues of hCETP transgenic mice. It also shows a robust elevation of HDL-C and reduction of low-density lipoprotein-cholesterol in physiological models.
As a researcher, you are now able to obtain BI-5756, along with its negative control BI-9313 completely free of charge. You will own all results you will generate with the molecules and may use them for your own publications.
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About BI-5756:
BI-5756 is a potent and polar cholesteryl ester transfer protein (CETP) inhibitor with improved solubility and reduced lipophilicity compared to other CETP inhibitors. It eliminates completely from fat tissues of hCETP transgenic mice 21 days after cessation of treatment. BI-5756 inhibits the transfer of a fluorescence labelled lipid from donor vesicles to LDL with an IC50 of 145.5 nM. Its enantiomer BI-9313 is available as a negative control and has low binding affinity to CETP.
About opnMe:
opnMe.com, the new open innovation portal of Boehringer Ingelheim, aims to accelerate research initiatives to enable new insights of disease biology in areas of high unmet medical need by sharing well-characterized molecules and offer collaborations for science. In the spirit of collaboration, our molecules are provided to the scientific community to help unlock and fulfill their full potential. These molecules are either freely available as “Molecules to Order” or applied via scientific research submissions such as our current “Molecules for Collaboration” call offering the HER2 exon20 Inhibitor. As part of our third pillar, our “opn2EXPERTS” program, we also enlist scientific advice on key biologic issues to fuel further drug discovery and deliver novel solutions that benefit unmet patient needs, such as our latest call on ECM degradation in NASH.