orlistat

Orlistat (Tetrahydrolipstatin) 是一种脂肪酶 (lipase) 抑制剂，也是一种脂肪酸合成酶 (FASN) 抑制剂。Orlistat 具有促减肥的作用。

Octyl Orlistat, 作为一种潜在的脂肪酸合成酶(FASN)抑制剂, 在减少肿瘤细胞增殖方面显示出显著成效。通过靶向FASN并引发细胞凋亡，Orlistat 正被研究用作抗肿瘤化合物。与Cerulenin和C75相比，Orlistat在细胞培养和细胞系中表现出更高的抑制效力。在LN229细胞中，使用200 µM Orlistat处理48小时后，细胞生长减少了63.9 ± 8.7%，而在LT68细胞中细胞生长的减少率为76.3 ± 23.7%。经Orlistat处理的器官型切片培养显示，在Ki67染色后增殖减少，并观察到caspase-3的增加剪切。

Isoleucine orlistat, L- is a bioactive chemical.

Orlistat degradation product is a degradation product of the digestive lipase inhibitor orlistat . It is formed via hydrolytic and thermal degradation as well as digestion by human carboxyl ester lipase.

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......

TAK-137 是一种 AMPA 受体增强剂,具有抗抑郁作用。TAK-137 具有改善认知的能力，可用于研究神经分裂症。