Metabolism

Sezolamide is a carbonic anhydrase inhibitor.

ICMT-IN-9 (compound 47) is a potent ICMT inhibitor with an IC50 value of 0.16 μM [1].

MeIm (compound 7), a peptide mimetic targeting PCSK9, exhibits cholesterol-lowering properties by enhancing the cellular uptake of LDL (EC 50 = 6.04 μM) and obstructing PCSK9's interaction with LDLR (IC 50 = 11.2 μM). This compound is useful for research in cardiovascular diseases.

<p>Gentisuric acid, an Aspirin metabolite and a substrate of α-amidating monooxygenase (PAM), mitigates DNA damage induced by Mitomycin C. [1] [2]</p>

FTI-2153 inhibits farnesyltransferase with 1.4 nM IC50, >3000x more effective on H-Ras than Rap1A.

Hydroxy lenalidomide, a metabolite of the thalidomide analog and anticancer agent lenalidomide, is a derivative substance involved in the metabolic process of its parent compound.

Cholesterol 24-hydroxylase-IN-2 is a potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), exhibiting an IC50 value of 5.4 nM, and has potential

Curcumin-β-D-glucuronide, a principal metabolite detected in hepatic tissue and portal blood following oral consumption of Curcumin, is utilized in colon cancer

FXIa-IN-1 is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.

UCPH-102: Selective EAAT1 inhibitor, IC50 0.43 μM, treats Alzheimer's, ALS, chronic pain, OCD; crosses blood-brain barrier, targets T-ALL cells.

Phenylpyropene C inhibits JAK/STAT and IFN-γ expression (IC50: 5.4-10.8 μM), also blocks acyl CoA (IC50: 16.0 μM).

GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).

8-isoProstaglandin F2α (8-isoPGF2α; 8-isoprostane) is a byproduct of non-specific lipid peroxidation, resembling prostaglandin in structure. In humans and rats, its metabolite, 12,3-dinor-8-isoPGF2α, is formed following exogenous administration of 8-isoPGF2α, which is converted to 2,3-dinor-8-isoPGF1α and 2,3-dinor-8-isoPGF2α. Additionally, rat hepatocytes can further break down 8-isoPGF2α into a β-oxidation product, 2,3,4,5-tetranor-8-isoPGF2α. The metabolite, 2,3-dinor-8-isoPGF2α, is normally found in human urine at concentrations of 200-300 pg/ml. Its levels rise in conditions associated with oxidative stress, such as smoking, demonstrating a correlation with the concentration of its precursor, 8-isoPGF2α.

ICMT-IN-36 (compound 40) serves as an ICMT inhibitor, with an IC50 value of 0.181 μM [1].

AZD7687: Selective DGAT1 inhibitor, IC50 of 80 nM. In vitro reduces postprandial TAG. In vivo significant GI side effects at >5 mg/day dose.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are a class of endogenous lipids whose levels are modulated by fasting and high-fat diets and are linked to insulin sensitivity. These compounds typically consist of a C-16 or C-18 fatty acid, such as palmitoleic, palmitic, oleic, or stearic acid, esterified to a hydroxylated C-16 or C-18 lipid. One specific form of FAHFA, known as 9-OAHSA, involves the esterification of oleic acid to 9-hydroxy stearic acid. Within the FAHFA family, OAHSAs notably represent the predominant form found in the serum of glucose-tolerant AG4OX mice, which uniquely overexpress the Glut4 glucose transporter in adipose tissue.

N-Desethyl Brinzolamide oxalate functions as a dual inhibitor targeting Carbonic anhydrase II and Carbonic anhydrase IV, exhibiting inhibitory concentrations (IC50) of 1.28 nM and 128 nM, respectively [1].

11-Dehydro Thromboxane B3 (11-dehydro TXB3) serves as a urinary metabolite of TXA3 in humans following an increased dietary intake of EPA.

1-Stearoyl-2-eicosapentaenoyl-sn-glycero-3-PC is a phospholipid comprising stearic acid and eicosapentaenoic acid at the sn-1 and sn-2 positions, respectively, identified in human red blood cells (RBCs).

Deleobuvir sodium (BI207127), a hepatitis C NS5B inhibitor, showed promise in some trials but was discontinued in 2013 due to insufficient efficacy.