esterases

Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.

AA26-9 is an effective and broad-spectrum inhibitor of serine hydrolase.

Aprotinin (Traskolan) is a broad-spectrum serine protease (BPTI) inhibitor that inhibits the activity of a number of different esterases and proteases. Aprotinin is an antifibrinolytic agent used to minimize hemorrhage during complex surgical procedures.

Aripiprazole lauroxil, the N-acyloxymethyl prodrug form of aripiprazole, a long-acting injectable (LAI) antipsychotic. Aripiprazole lauroxil is cleaved by esterases in vivo to N-hydroxymethyl aripiprazole (lauric acid), which is then cleaved to aripiprazole, which is non-toxic.

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), is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.

Gemcitabine elaidate (CP-4126) hydrochloride is a lipophilic pro-drug of Gemcitabine, converted to Gemcitabine by esterases for phosphorylation. Unlike gemcitabine, Gemcitabine elaidate hydrochloride can be administered orally, displaying schedule and dose-dependent toxicity and antitumor activity.

Tamethicillin is an ester prodrug of methicillin (MET) that is converted to MET in the body by non-specific esterases.

5-Hydroxymethyl tolterodine (formate) (PNU-200577 (formic)) is an active metabolite of the muscarinic acetylcholine receptor antagonists Tolterodine and Fesoterodine. It is synthesized by the cytochrome P450 (CYP) isoenzyme CYP2D6 and plasma esterases.

Fosfenopril (Fosinoprilat) is a potent angiotensin-converting enzyme (ACE) inhibitor that mitigates lipopolysaccharide-induced inflammation in monocytes through the suppression of TLR4/NF-κB signaling pathways, and Fosfenopril is utilized in cardiovascular and anti-inflammatory research to investigate molecular mechanisms of ACE inhibition.

(R,S,S,S)-Orlistat is a stereoisomeric derivative of orlistat (Tetrahydrolipstatin; THL) that inhibits three mycobacterial lipid esterases: Ag85C (KI: 16.43 μM), Rv3802 (EC50: 16.2 nM), and Pks13-TE.

TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of excitatory amino acid transporters (EAAT). It is capable of crossing cell membranes and is activated by hydrolysis from endogenous cellular esterases to form an active EAAT inhibitor. TAOA AM Ester trimethyl lock is useful for studying neurodegeneration and neuronal cell death.

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 (SR 26334) is a major inactive metabolite of clopidogrel, accounting for 85% of circulating clopidogrel, and is produced by hydrolysis by esterases. CLPM is commonly used as a reference standard for metabolic analysis of clopidogrel.

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.

Isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. Isavuconazole binds to and inhibits the fungal cytochrome P450 family enzyme lanosterol 14-alpha-demethylase (CYP51), which catalyzes the demethylation of

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.