Daglutril, a NEP ECE inhibitor, is potentially used for the treatment of hypertension, heart failure andpulmonary. Daglutril inhibits systemic conversion of big endothelin-1 in humans.
Vildagliptin carboxylic acid metabolite is the major metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor vildagliptin in humans. Vildagliptin carboxylic acid metabolite has an IC50 value of 477 μM for DPP-4 in human Caco-2 cells. It is formed from hydrolysis of the cyano group on vildagliptin.
Vildagliptin dihydrate (LAF237 dihydrate) is a powerful and stable dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating selectivity with an IC50 of 3.5 nM in human Caco-2 cells. This compound exhibits exceptional oral bioavailability and significant antihyperglycemic activity [1].
PNU-EDA-Gly5 is a DNA topoisomerase I inhibitor-based oligo-glycine linker-payload used for the synthesis of antibody-drug conjugates (ADCs). It consists of the DNA topoisomerase I inhibitor PNU-159682 and the linker EDA-Gly5.
KT109 is a selective inhibitor of DAGLβ (IC50 = 42 nM). KT109-treated wild-type mice displayed reductions in LPS-induced allodyni as well as in DAGL-β (- -) micea. Repeated KT109 administration prevented the expression of LPS-induced allodynia, without ev