SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.
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......