hepatic enzyme

Selective tryptophan 2, 3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). Exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. Reduces growth of TDO-expressing P

Docetaxel trihydrate (RP-56976 Trihydrate) is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme elevations and rarely to instances of acute hepatic necrosis generally due to severe hypersensitivity reactions or sepsis.

D-Glucaric acid potassium (D-Saccharic acid potassium salt) is a compound formed from oxidizing sugars, which can be used to test for the presence of hepatic enzyme induction. Studies indicate that D-glucuronolactone dehydrogenase oxidizes D-Saccharic acid potassium salt into D-glucaro-l,4;6,3-dilactone. Alternate studies suggest that D-Saccharic acid potassium salt forms a complex with Cu(II) and H2O2to decolorize azo, acridine, triphenyl methane, anthraquinone and thiazine-based dyes.

1. Peimisine (Ebeiensine) can affect M-receptor, excit β-receptor, restrain the release of internal calcium, and promote to releaseing nitrogen monoxidum in order to relax tracheal smooth muscle and relieve asthma. 2. Peimisine can attenuate lung tissue injury( ALI), LDH and MDA amount in ALI mice in a dose dependent manner, it also lower the total protein, total white blood cells, lymphocyte and neutrophilic leukocyte in bronchoalveolar lavage fluid( BALF); suggests that peimisine can play a protective role against LPS-induced acute lung injury. 3. Peimisine has the protective effect on the experimental hepatic fibrosis formation, the possible mechanisms are associated with inhibiting fibrogenesis and fibrosis accumulation, and decreasing lipid peroxidation. 4. Peimisine can inhibit angiotensin I converting enzyme activity in a dose-dependent manner, displaying 5 % inhibitory concentration values of 526.5 microM, thus, it may have antihypertensive action.

(R)-3-Hydroxy Midostaurin is a potent inhibitor of kinases,is a major metabolite of midostaurin undergoing by the hepatic CYP3A4 enzyme,has the potential for acute myeloid leukemia (AML).

Flumecinol is a hepatic enzyme (cytochrome P-450 monooxygenases) inducer.

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3',5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3'-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

HIV-1 inhibitor-16 (compound 7a) is a potent HIV-1 inhibitor with an EC50 of 1.3 nM against wild-type HIV-1, and exhibits inhibitory activity against HIV-1 K103N, E138K, Y181C, and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM, and 35 nM, respectively. It demonstrates good solubility, hepatic microsomal stability, and lacks significant CYP enzyme inhibitory activity or acute toxicity.

Moexipril hydrochloride (Moexipril HCl) is a potent orally active nonsulfhydrylangiotensin converting enzyme (ACE)inhibitor, used for the treatment of hypertension and congestive heart failure.

Cinnamic acid, hydrazide is an unsaturated carboxylic acid and precursor to aspartame via enzyme-catalysed amination to phenylalanine. Cinnamic acid may be useful in prevention or treatment of Diabetes through various mechanism of actions including stimulation of insulin secretion, improvement of pancreatic β-cell functionality, inhibition of hepatic gluconeogenesis, enhanced glucose uptake, increased insulin signaling pathway, delay of carbohydrate digestion and glucose absorption, and inhibition of protein glycation and insulin fibrillation.

Nedosiran sodium, a GalNAc-dsRNA conjugate, is engineered to suppress the synthesis of the hepatic lactate dehydrogenase (LDH) enzyme.

Glucagon significantly impacts protein and amino acid metabolism. It hinders the integration of amino acids into the proteins of the liver, muscle, and pancreas, augmenting nitrogen excretion and stimulating hepatic urea synthesis. Additionally, it elevates hepatic transaminase and urea cycle enzyme levels. Glucagon also enhances hepatic amino acid uptake, facilitating their conversion into liver glycogen, and reduces blood amino acid concentrations [1].

Compound 6k, also known as Anti-hepatic fibrosis agent 2, is an orally active inhibitor of the COL1A1 enzyme and exerts anti-fibrogenic effects by targeting the Ewing sarcoma breakpoint region 1 (EWSR1)[1].