hepatic enzyme

LM10 是有效的色氨酸 2,3-双加氧酶的抑制剂。色氨酸 2,3-双加氧酶是一种无关的肝酶，它可通过犬尿氨酸途径降解色氨酸。它对研究癌症疾病具有潜在的研究价值。

Docetaxel trihydrate (RP-56976 Trihydrate) 是一种抗肿瘤试剂，抑制微管解聚的IC50值为 0.2 μM。它是紫杉醇的半合成类似物，能减弱 bcl-2 和 bcl-xL 基因表达的影响。它阻滞G2 M 细胞周期，导致细胞凋亡。

D-Glucaric acid potassium (D-Saccharic acid potassium salt) 是内源性代谢产物的一种。

Peimisine (Ebeiensine) 非竞争性拮抗气管平滑肌 M 受体，抑制 Ach 引起的平滑肌收缩。它兴奋 β 受体和拮抗内钙释放，促进一氧化氮释放，可舒张气管平滑肌，有平喘作用。

(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) 是一种高效的 HIV-1抑制剂，对野生型 HIV-1 的 EC50为 1.3 nM。HIV-1 inhibitor-16 对 HIV-1 K103N、E138K、Y181C 和 L100I 病毒株也有一定的抑制活性，EC50分别为 5.4 nM、9.2 nM、22 nM 和 35 nM。HIV-1 inhibitor-16 具有良好的溶解性和肝微粒体稳定性，未表现出明显的 CYP 酶抑制活性或急性毒性。

Moexipril hydrochloride (Moexipril HCl) 是一种有口服活性的，不含巯基的血管紧张素转化酶抑制剂，可治疗高血压和充血性心力衰竭。

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 是一种靶向乳酸脱氢酶 (LDH)的 RNA 干扰剂 (RNAi)。Nedosiran sodium?可用于研究并发终末期肾病 (ESRD)的原发性高草酸尿症 (PH)。

Glucagon 对蛋白质和氨基酸的代谢产生显著的调节作用。它抑制了氨基酸与肝脏、肌肉以及胰腺蛋白的结合，增加氮的排出，并促进肝脏内尿素的合成。同时，Glucagon 增加了肝脏中转氨酶和尿素循环酶的浓度，提高了肝脏对氨基酸的摄取，并加强了氨基酸与肝糖原之间的结合，从而降低了血液中的氨基酸浓度。

Fibrosis agent 2为针对Ewing肉瘤断点区域1 (EWSR1) 的特定抗纤维化化合物。

ELOVL6-IN-5（compound B）是针对ELOVL6的抑制剂，后者为长链脂肪酸家族6的延长酶，负责饱和及单不饱和长链脂肪酸的延长，并且是糖尿病治疗中的有效靶点。此化合物能在饮食诱导肥胖（DIO）的小鼠模型中有效降低肝脏脂肪酸水平，尽管如此，通过ELOVL6-IN-5引起的ELOVL6抑制并未改善胰岛素抵抗问题。