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.
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.
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.
(R)-KT109 is the (R) isomer of the diacylglycerol lipase β (DAGLβ) inhibitor KT109 . (R)-KT109 is an inhibitor of DAGLβ (IC50 = 0.79 nM) and of DAGLα-mediated hydrolysis of 1-stearoyl-2-arachidonoyl-sn-glycerol . It also inhibits α β-hydrolase domain-containing protein 6 (ABHD6) with an IC50 value of 2.51 nM. (R)-KT109 is more potent at DAGLβ, DAGLα, and ABHD6 than (S)-KT109 .
(S)-KT109 is the (S) isomer of the diacylglycerol lipase β (DAGLβ) inhibitor KT109 . (S)-KT109 is a less potent inhibitor of DAGLβ (IC50 = 39.81 nM), DAGLα-mediated hydrolysis of 1-stearoyl-2-arachidonoyl-sn-glycerol (IC50 = 794.3 nM), and α β-hydrolase domain-containing protein 6 (ABHD6; IC50 = 630.9 nM) than (R)-KT109 .
Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg kg) decreases serum cholesterol levels and total bod......