Metabolism

α-Glucosidase-IN-13 is an inhibitor of α-glucosidase (IC50: 5.69 μM).

GPX4 9i is a ferroptosis inducer that exhibits cytotoxicity towards HT-1080 cells, with an IC50 of 0.007 µM. This cytotoxic effect can be mitigated by the use of the ferroptosis inhibitor, ferrostatin-1.

GNTI TFA is a selective kappa opioid receptor antagonist.

Mesembrine is a serotonin reuptake inhibitor and is also a weak inhibitor of the enzyme phosphodiesterase 4 (PDE4).

Dibutyl phosphate (DBUP) is a metabolite of organophosphate esters (OPEs) found in urine. The presence of dibutyl phosphate is positively correlated with an increased risk of sarcopenia.

Retezorogant is a retinoic acid receptor-related orphan receptor gamma (RORγ) antagonist.

1-Stearoyl-sn-glycerol 3-phosphate sodium, a biologically active phospholipid, plays a crucial role in regulating cell motility, proliferation, invasion, survival, and the production of growth factors through interactions with G protein-coupled receptors (GPCR). Synthesized during the formation of membrane phospholipids, this compound typically has a low plasma concentration (approximately 100nM) and originates from various cell types, including activated platelets, epithelial cells, leukocytes, neuronal cells, and tumor cells. Its distinctive structure features stearic acid at the sn-1 position and a hydroxyl group at the sn-2 position.

SCP1-IN-2: potent, selective SCP1 inhibitor; induces REST degradation, hinders its activity, may study REST-driven glioblastoma growth.

C16-18:1 PE is a lipid known for its role in facilitating membrane fusion and enhancing endosomal escape, significantly boosting mRNA delivery efficiency. This compound is utilized in the synthesis of lipid nanoparticles (LNP).

FXR agonist12 (Compound C7) is an orally active FXR agonist. It downregulates bile acid synthesis-related genes and upregulates bile acid transport-related genes in HepG2 cells. FXR agonist12 alleviates ANIT-induced cholestasis and reduces liver damage and fibrosis in a mouse model of NASH.

α-Glucosidase-IN-18 (7B) is an orally active inhibitor of α-glucosidase, displaying an IC 50 value of 3.96 μM.

ZK159222 is an effective 1α,25-(OH)2D3 receptor (VDR) agonist. ZK159222 has a partial agonistic character.

EB-0156: potent ER α-glucosidase inhibitor, IC50 of 0.0479/ <0.001 μM, N-substituted valerian, broad-spectrum antiviral potential.

EtoricoxibN1'-oxide is a metabolite of Etoricoxib. It does not inhibit COX-1 and does not significantly inhibit COX-2.

Implitapide is an inhibitor of microsomal triglyceride transfer protein (MTP).

MolPort-010-778-422 is a high-affinity inhibitor targeting the ACE2 receptor of the SARS-CoV-2 virus. It demonstrates remarkable antiviral activity with an IC50 of 8.9 nM and holds promise for use in studies related to SARS-CoV-2.

ONL-1204 is a small molecule, CD95 antigen inhibitor (Fas inhibitor) being developed by ONL Therapeutics for the treatment of retinal detachment.

TAK-915: potent, brain-ready PDE2A inhibitor, 0.61 nM IC50, 4100x selectivity over PDE1A.

PTP1B-IN-16: selective benzimidazole inhibitor of PTP1B, Ki: 12.6 μM, potential for type 2 diabetes research.