6bK (TFA)

6bK TFA is a selective insulin-degrading enzyme (IDE) inhibitor with an IC₅₀ of 50 nM. 6bK TFA binds to the distal pocket of IDE, thereby blocking substrate binding, peptide unfolding and cleavage processes, and reducing the degradation of insulin, glucagon and amylin. 6bK TFA improves oral glucose tolerance but impairs intraperitoneal glucose tolerance. 6bK TFA can be used in research related to type 2 diabetes^[1][2]. IC50 & Target:IC₅₀: 50 nM (IDE)^[1] In Vitro:6bK TFA potently inhibits IDE activity with an IC₅₀ of 50 nM^[2].
6bK (1 h) TFA exhibits a high plasma protein binding rate, as well as favorable 1-hour stability in mouse plasma and microsomes^[2]. In Vivo:Single-dose 6bK TFA improves oral glucose tolerance in lean mice and high-fat diet-fed mice (with a more pronounced effect in high-fat diet-fed mice), but induces glucose intolerance when glucose is administered intraperitoneally^[1].
Acute inhibition of insulin-degrading enzyme by 6bK (40-90 mg/kg) TFA improves oral glucose tolerance in lean and DIO mice, delays gastric emptying via the amylin signaling pathway, impairs intraperitoneal glucose tolerance via the glucagon signaling pathway, and enhances insulin-mediated hypoglycemic responses, all of which depend on IDE activity^[2].
6bK (80 mg/kg; i.p.; single administration) TFA exhibits a potentiated hypoglycemic response to insulin injection in mice^[2].