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].
In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC50 = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (IC50s > 10 μM) and does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 μM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-dependently inhibit high-fat diet intake and reduce body weight.
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.
Body Protection Compound 157 (BPC 157) is a pentadecapeptide derived from BPC, identified in gastric juice, exhibiting diverse biological activities. At 2 µg/ml, BPC 157 enhances primary rat tendon fibroblast cell migration and F-actin formation. Furthermore, doses of 0.01 and 10 µg/kg, intraperitoneally (i.p.), mitigate paw swelling, bone erosion, and mononuclear cell infiltration in the joints of rats with rheumatoid arthritis induced by complete Freund's adjuvant (CFA). It also diminishes gastric ulcer size in rats caused by indomethacin, aspirin, or diclofenac at these doses. Additionally, BPC 157 reduces catalepsy duration and tremor severity in a mouse model of Parkinson's disease triggered by MPTP.
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