daglβ-in-1

DAGLβ-IN-1，一种针对二酰基甘油脂肪酶 β (DAGLβ) 的抑制剂，可用作DAGL特异性活性探针的通用中间体。

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.

Orlistat-D3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat (T0686) 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 (T0686)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 (T0686) (10 mg/kg)decreases serum cholesterol levels and total bod......