hydrolases

LY2183240 是大麻素摄取阻滞剂。它是内源性大麻素降解酶脂肪酸酰胺水解酶的有效共价抑制剂。它抑制脂肪酸酰胺水解酶 (FAAH) 活性，IC50 为12.4 nM。它也抑制其他几种脑丝氨酸水解酶，对 MAG 脂肪酶、bh6 和 KIAA1363 的 IC50分别为 5.3、0.09 和 8.2 nM。

LEI110 是一种有效的 Phospholipase A2, group XVI (PLA2G16) 抑制剂，Ki 值为 20 nM。 LEI110 是 HRASLS 硫醇水解酶家族（即 PLA2G16、HRASLS2、RARRES3 和 iNAT）的选择性泛抑制剂。

BSH-IN-1 是一种重组的肠道细菌胆汁盐水解酶 (BSHs) 的有效和共价抑制剂，对 B. longum BSH (革兰氏阳性) 和 B. theta BSH (革兰氏阴性菌) 的 IC50 分别为 108 和 427 nM。

ABC47 是一种高效的丝氨酸水解酶 (serine hydrolases) 抑制剂，对ABHD4和ABHD3的IC50分别为0.03 μM和0.1 μM。在研究婴儿神经元蜡样脂褐素沉积症方面，ABC47 发挥了重要作用。

The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The calcium-independent phospholipases (iPLA2) are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA2β except at high doses of 20-30 μM. (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM.

Epoxide hydrolases convert the EETs into vicinal diols, with the concurrent loss of much of their biological activity. The 8(S),9(R)-EET isomer is metabolized by platelet COX to form 8(S),9(R),11(R)-THETA, a trihydroxy fatty acid which may act as a renal vasoconstrictor.

Eicosapentaenoic acid is an ω-3 polyunsaturated fatty acid that is abundant in marine organisms and fish oils. EPA is metabolized, in part, through cytochrome P450-catalyzed epoxidation followed by conversion to the vicinal diols by epoxide hydrolases. (±)5(6)-DiHETE is a possible metabolite produced from EPA following epoxidation of the α-5 double bond. The biological activity of (±)5(6)-DiHETE has not been documented.

Eicosapentaenoic acid is metabolized, in part, through cytochrome P450-catalyzed epoxidation followed by conversion to the vicinal diols by epoxide hydrolases. (±)5(6)-DiHETE is a possible metabolite produced from EPA following epoxidation of the α-5 double bond. (±)5(6)-DiHETE lactone is a 1,5 cyclic ester derived from (±)5(6)-DiHETE. While its biological activity is unknown, the selective capacity of (±)5(6)-DiHETE to form this lactone can be utilized to specifically quantify (±)5(6)-DiHETE in biological samples.

(±)-11(12)-DiHET is an oxylipin. 11(S),12(S)-DiHET and 11(R),12(R)-DiHET are vicinal diols formedviaenzymatic hydration of 11(12)-EET by cytosolic or soluble epoxide hydrolases in a non-stereoselective manner.1,2,3(±)11(12)-DiHET MaxSpec standard is a quantitative grade standard of (±)11(12)-DiHET that has been prepared specifically for mass spectrometry and related applications where quantitative reproducibility is required. The solution has been prepared gravimetrically and is supplied in a deactivated glass ampule sealed under argon. The concentration was verified by comparison to an independently prepared calibration standard. This (±)11(12)-DiHET MaxSpec standard is guaranteed to meet identity, purity, stability, and concentration specifications and is provided with a batch-specific certificate of analysis. Ongoing stability testing is performed to ensure the concentration remains accurate throughout the shelf life of the product.Note: The amount of solution added to the vial is in excess of the listed amount. Therefore, it is necessary to accurately measure volumes for preparation of calibration standards. Follow recommended storage and handling conditions to maintain product quality.

Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-1509 (1995).2. Morisseau, C., Newman, J.W., Dowdy, D.L., et al. Inhibition of microsomal epoxide hydrolases by ureas, amides, and amines. Chem. Res. Toxicol. 14(4), 409-415 (2001).3. Jain, M.K., Ghomashchi, F., Yu, B.Z., et al. Fatty acid amides: scooting mode-based discovery of tight-binding competitive inhibitors of secreted phospholipases A2. J. Med. Chem. 35(19), 3584-3586 (1992). Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1 References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-1509 (1995).2. Morisseau, C., Newman, J.W., Dowdy, D.L., et al. Inhibition of microsomal epoxide hydrolases by ureas, amides, and amines. Chem. Res. Toxicol. 14(4), 409-415 (2001).3. Jain, M.K., Ghomashchi, F., Yu, B.Z., et al. Fatty acid amides: scooting mode-based discovery of tight-binding competitive inhibitors of secreted phospholipases A2. J. Med. Chem. 35(19), 3584-3586 (1992).

JCP678 is an irreversible serine hydrolases inhibitor.

AB05831, also known as 2-Acetamido-1,2-dideoxynojirimycin, is a highly potent and specific inhibitor of beta-hexosaminidase. N-Acetyl-3-hexosaminidase (HEX) is a member of lysosomal hydrolases, which catalyzes hydrolysis of terminal, non-reducing N-acetyl-|3-D-glucosamine (GlcNAc) andN-acetyl-(3-D-galactosamine (GalNAc) residues in glycoproteins, gan-gliosides, and glycosaminoglycans (GAGs). HEX, released by chondrocytes into the extracellular compartment, promotes cartilage matrix degradation. Osteoarthritis patients have increased HEX activity in synovial fluid.

JZP-MA-13是一种选择性α β-水解酶结构域6 (ABHD6) 抑制剂，其IC50值为392 nM。该化合物对MAGL、ABHD12、FAAH或其它丝氨酸水解酶不表现出抑制作用。JZP-MA-13还被用作ABHD6在体内成像的正电子发射断层扫描(PET)配体。

Enzyme-IN-1（compound 1）为基于肽的N端亲核试剂（Ntn）水解酶抑制剂，特别针对20S蛋白酶体的糜胰蛋白酶样活性（CT-L）进行抑制，可能展现出抗炎特性。

Carboxylesterase (CESs), 即羧酸酯水解酶，广泛分布于自然界，常见于哺乳动物肝脏，常用于生化研究。Carboxylesterase 催化多种内源和外源底物的水解，包括酯、硫酯、氨基甲酸酯和酰胺，使羧酸酯水解成相应的醇和羧酸。

5(6)-DiHET is a racemic compound synthesized through the action of epoxide hydrolases on 5(6)-EET, encompassing both enantiomeric forms. It serves as a quantitative marker for 5(6)-EET, facilitating its measurement by utilizing the compound's conversion to 5(6)-δ-lactone in solution. Additionally, 5(6)-DiHET activates large-conductance calcium-activated potassium (KCa1.1 BK) channels in rat small coronary artery smooth muscle cells, supporting its biological significance in vascular regulation. It also acts as a substrate for sheep seminal vesicle COX, leading to the in vitro production of 5,6-dihydroxy prostaglandin E1 and F1α metabolites. Notably, its levels diminish in the plasma of rats subjected to a high-fat diet, indicating a potential role in the pathophysiology of hyperlipidemia.

WWL229 是羧酸酯酶3的选择性抑制剂 (IC50:1.94 µM) 。它可作用于培养脂肪细胞，提高脂质的储存，并减少基础脂肪分解。

D-Glucopyranose, 98% (α-Sophorose, 98%) 是一种底物，适用于多种糖苷水解酶如α-葡萄糖苷酶，并用于糖生物学的研究。

2′-Hydroxy-5′-nitrohexadecanamide 是一种溶酶体水解酶 (Lysosomal hydrolase) 的抑制剂，其结构包含十五酸和末端硝基苯酚的脂质。通过抑制溶酶体水解酶的活性，它会导致细胞内脂质的积累。此外，2′-Hydroxy-5′-nitrohexadecanamide 还可以用来合成用于测定鞘磷脂酶活性的显色底物。