α/β-hydrolase-in-1

α/β-Hydrolase-IN-1 demonstrates exceptional potency, with MICs of 50 μM (25 μg/mL) against M. smegmatis and 16 μM (8.4 μg/mL) against M. tuberculosis H37Ra, establishing it as a superior compound in this class.

JZP-MA-11 is a positron emission tomography (PET) ligand that specifically targets the endocannabinoid α β-hydrolase domain 6 (ABHD6) enzyme. It exhibits selective inhibition of ABHD6 with an IC50 value of 126 nM and can cross the blood-brain barrier (BBB). The compound, labeled with [18F], shows promising potential for preclinical evaluation in mice and nonhuman primates (NHP) as a tool for investigating brain ABHD6 activity [1].

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......

mEH-IN-1 (Compound 62) is a potent inhibitor of microsomal epoxide hydrolase (mEH), with an IC50 value of 2.2 nM. This α β-fold hydrolase enzyme is widely expressed in mammalian tissues and primarily localized in the endoplasmic reticulum (ER) of eukaryotic cells, responsible for hydrolyzing various epoxide-containing molecules. Research on mEH-IN-1 can enhance the understanding of preeclampsia, hypercholanemia, and cancer [1].

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.