esterases

Etilevodopa hydrochloride (L-DOPA ethyl ester) 是 Levodopa 的前药，在胃肠道中被非特异性酯酶快速水解产生 Levodopa 和乙醇。Levodopa 是多巴胺的前体，有助于中枢神经系统的渗透和传递多巴胺。Etilevodopa HCl 可用于帕金森病 (PD)的相关研究。

AA26-9 是广谱丝氨酸水解酶的高效抑制剂。它的靶点包括丝氨酸肽酶、酰胺酶、脂肪酶、酯酶和硫酯酶。在永生化 T 细胞系，检测到它对 40+ 丝氨酸水解酶中的 1 3 有抑制作用。

Aprotinin (Traskolan) 是一种广谱丝氨酸蛋白酶 (BPTI) 抑制剂，可抑制多种不同酯酶和蛋白酶的活性。Aprotinin 是一种抗纤溶剂，用于减少复杂手术中的出血。

Isavuconazonium sulfate 是一种口服活性抗真菌药，是活性三唑类抗真菌药物 Isavuconazole 的前药，可用于侵袭性曲霉菌病和毛霉菌病。

Aripiprazole lauroxil 是一种长效注射剂 (LAI) 的抗精神病药物，是阿立哌唑的 N-酰氧基甲基前药形式。它能够被体内酯酶裂解为 N-羟甲基阿立哌唑(月桂酸)，再裂解为阿立哌唑，无毒性。

Etilevodopa is an ethyl-ester prodrug of Levodopa which is used for the treatment of Parkinson's disease (PD). It is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Levodopa is the direct precursor of dop

Gemcitabine elaidate (CP-4126) 是 Gemcitabine 的亲脂性前药。它通过酯酶转化为 Gemcitabine 以被磷酸化。它具有抗肿瘤活性。

Gemcitabine elaidate (CP-4126) hydrochloride 是 Gemcitabine 的亲脂性前药。Gemcitabine elaidate hydrochloride 通过酯酶转化为 Gemcitabine 以被磷酸化。Gemcitabine elaidate hydrochloride 可以口服给药，具有抗肿瘤活性。

Tamethicillin是methicillin (MET)的基础酯类前药，通过体内的非特异性酯酶转化为MET。

5-Hydroxymethyl tolterodine (formate) (PNU-200577 (formic)) 是毒蕈碱乙酰胆碱受体拮抗剂Tolterodine和Fesoterodine的活性代谢物。此化合物通过细胞色素P450 (CYP) 的同工酶CYP2D6和血浆酯酶合成。

Fosinoprilat, an active phosphinic acid metabolite of prodrug fosenopril, is activated by esterases in vivo. Fosinoprilat binds zinc with phosphinic acid group.

Lorajmine, a monochloroacetyl derivative of ajmaline, is a class Ia antiarrhythmic agent that is rapidly hydrolyzed to ajmaline by plasma and tissue esterases.

AM7499 is a non-selective cannabinoid receptor agonist with remarkably high in vitro and in vivo potency. It is readily hydrolysed by plasma esterases and to be less prone to deposition in bodily fat than existing classical cannabinoid agonists.

Dabigatran acyl-β-D-glucuronide is a major active metabolite of the thrombin inhibitor dabigatran . The prodrug of dabigatran, dabigatran etexilate , is hydrolyzed by plasma esterases to form dabigatran, which is metabolized primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT2B15 to form dabigatran acyl-β-D-glucuronide. Dabigatran acyl-β-D-glucuronide increases activated partial thromboplastin time (aPTT) in isolated human platelet-poor plasma equipotently to dabigatran.

Clopidogrel Carboxylic Acid hydrochloride(氯吡格雷酸盐酸盐)是一种氯吡格雷的主要无活性代谢产物，占85%的循环氯吡格雷，由酯酶水解生成。CLPM常用于氯吡格雷代谢分析的参考标准物。

In addition to its role in the Krebs cycle, α-ketoglutarate (2-oxoglutarate) has roles as a substrate or modulator of enzymes. 5-Octyl-α-ketoglutarate, also known as α-ketoglutarate octyl ester, is a stable, cell-permeable molecule that generates free α-ketoglutarate upon hydrolysis of the ester bond by cytoplasmic esterases. It is used in experiments to increase levels of intracellular α-ketoglutarate. 5-Octyl-α-ketoglutarate has been shown to modulate a variety of enzymes and signaling pathways, particularly in the context of glycolysis, hypoxia, and cancer.

Resolvin D1 is produced physiologically from the sequential oxygenation of docosahexaenoic acid by 15- and 5-lipoxygenase . It reduces human polymorphonuclear leukocyte transendothelial migration, the earliest event in acute inflammation, with an EC50 value of ~30 nM. RvD1 methyl ester is a methyl ester version of the free acid that may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracellular esterases, leaving the free acid.

Resolvin D2 (RvD2) is a lipid mediator biosynthesized by the sequential oxygenation of docosahexaenoic acid by 15- and 5-lipoxygenase. It evokes diverse anti-inflammatory effects which may mediate the resolution of inflammation. RvD2 methyl ester is a methyl ester version of the free acid which may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracellular esterases, leaving the free acid.

Resolvin D3 methyl ester is a methyl ester version of the free acid that may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracellular esterases, leaving the free acid.

Prostaglandin E2 (PGE2) isopropyl ester is a more lipophilic form of the free acid, PGE2. PG esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid by endogenous esterases upon in vivo administration, making the esters useful prodrugs. In general, the C-1 esters of PGs show greatly diminished receptor activity in vitro compared to the parent free acids.

Esterastin is an Inhibitor of esterases.

Cefditoren Pivoxil is a semi-synthetic, broad-spectrum, beta-lactamase resistant, third-generation cephalosporin antibiotic with bactericidal activity. Cefditoren pivoxil is a prodrug that is rapidly hydrolyzed by intestinal esterases during absorption to the microbiologically active cefditoren, an active aminothiazolyl cephalosporin. Cefditoren inactivates penicillin binding proteins (PBPs) thereby interfering with peptidoglycan synthesis and inhibiting bacterial cell wall synthesis.

Clofibric acid-d4 is intended for use as an internal standard for the quantification of clofibric acid by GC- or LC-MS. Clofibric acid is a peroxisome proliferator-activated receptor α (PPARα) agonist (EC50 = 50 µM in a transactivation assay) and the active metabolite of clofibrate. It is formed from clofibrate by tissue and serum esterases. Dietary administration of clofibric acid (0.067-0.22%) reduces serum cholesterol, phospholipid, and triglyceride levels in rats. It decreases glutamate oxaloacetate transaminase (GOT) levels and increases glutamate pyruvate transaminase (GPT) and lactate dehydrogenase (LDH) levels, markers of xenobiotic stress, in the plasma of carp (C. carpio) when administered in tank water at a concentration of 10 µg L. Clofibric acid has been found in wastewater effluent.

17(R)-Resolvin D1 (17(R)-RvD1) is an aspirin-triggered epimer of RvD1 that equivalently inhibits human polymorphonuclear leukocyte migration across the endothelium (EC50= ~30 nM), a precursor to acute inflammation. Unlike RvD1, it resists rapid degradation by eicosanoid oxidoreductases. In a mouse peritonitis model, 17(R)-RvD1 dose-dependently reduces leukocyte infiltration, achieving up to a 35% decrease with a 100 ng dose. Additionally, its methyl ester derivative, designed to enhance its pharmacokinetic and distribution properties as a more lipophilic prodrug, can be converted back into the active acid form by intracellular esterases.