29 July 2024
Excessive fructose consumption is associated with metabolic disorders such as obesity, diabetes and non-alcoholic fatty liver disease (NAFLD). Ketohexokinase (KHK) is an enzyme catalyzing the first committed step in fructose metabolism, by phosphorylating fructose into fructose-1-phosphate in an insulin-independent fashion. Animal model studies have demonstrated a reduction of fatty acid synthesis and liver steatosis upon KHK inhibition, rendering it an attractive target for the study of metabolic dysfunction.
BI-9787 is a selective KHK inhibitor, displaying equal potency for both KHK isomorphs, KHK-A and KHK-C. In addition, both BI-9787 and its negative control BI-2817 show good cell permeability and are suitable for in vitro as well as in vivo studies. As part of Boehringer Ingelheim’s commitment to open science, both compounds are now available to order for free on opnMe.com, with no IP restrictions. You retain full ownership and control of your results, which we encourage you to publish.
No registration required
Subscribe to our newsletter to stay updated as we add new molecules to opnMe.com.
About BI-9787:
BI-9787 is a zwitterionic KHK inhibitor, combining high permeability with a favorable oral rat PK and high target selectivity. It displays equal potency against both KHK isoforms with an IC50 of 12 nM against human KHC-A and 13 nM against human KHK-C. The negative control BI-2817 is structurally very close to BI-9787 and displays almost identical in vitro PK parameters.
About opnMe:
opnMe.com, the open innovation portal of Boehringer Ingelheim, fosters science and collaboration initiatives in areas of high unmet medical need. With our “Molecules to Order”, we share well-characterized tool compounds free of charge with no IP strings attached. These are complemented by the “Molecules for Collaboration” program, where we offer access to unprecedented molecules, with the chance to get your research proposal funded. Through our “opn2EXPERTS” and “techMATCH” programs, we enlist scientific advice on key scientific challenges to fuel further drug discovery and deliver novel solutions that address unmet patient needs. Our newly launched “opn2TALENTS” postdoc grants offers opportunities for high-level talents to pitch their scientific ideas and approaches for a well-defined research question, and to conduct their research at one of our discovery research sites in Germany, Austria, or the US.