daglα

DO34 analog is a triazole-based inhibitor of DAGL(α).

DO34 is a selective and potent diacylglycerol lipase (DAGL-α β) inhibitor that impairs fear extinction in mice, and can be used to study lipopolysaccharide inflammatory pain.

DH376 inhibits DAGLα in a time and dose dependent manner in mouse brain. DH376 shows picomolar activity.

(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......