Metabolism

AR453588 is an orally bioavailable anti-diabetic glucokinase activator (EC50: 42 nM) with anti-hyperglycemic activity.

YG1702, a potent inhibitor specific to ALDH18A1, suppresses the proliferation of MYCN-amplified neuroblastoma (NB) and reduces MYCN expression.

LY-338979 is an impurity of pemetrexedone.

Arachidonoyl amide (AMC-AA) is a fatty acid amide among several that serve to quantify fatty acid amide hydrolase (FAAH) activity. FAAH, with its relative lack of selectivity, processes various amide head groups beyond ethanolamine, the head group of its primary endogenous substrate, anandamide (AEA). The interaction of AMC-AA with FAAH leads to the liberation of fluorescent aminomethyl coumarin, which has an absorption peak at 360 nm and emission at 465 nm. This fluorescence release facilitates the rapid and efficient assessment of FAAH activity through the utilization of either a standard cuvette or a microplate fluorometer.

"Oral FXR antagonist 1 selectively blocks intestinal FXR, with IC50 of 2.1 μM, aiding in NASH research by improving liver health."

E-5324 is potent cholesterol acyltransferase (ACAT) inhibitor (IC50s: 44 to 190 nM).

Tetramyristoylcardiolipin (TMCL), an anionic lipid, plays a crucial role in studying cell membrane function and drug delivery mechanisms [1].

ICMT-IN-34 (compound 39) serves as an effective inhibitor of ICMT, exhibiting an IC50 value of 0.17 μM [1].

13-OAHSA, a branched fatty acid ester of hydroxy fatty acids (FAHFAs), results from the esterification of oleic acid to 13-hydroxy stearic acid. It represents a significant component of the FAHFA family, most abundantly expressed in the serum of glucose-tolerant AG4OX mice that exhibit adipose tissue-specific overexpression of the Glut4 glucose transporter. Similar to other FAHFAs which are known to enhance glucose tolerance, stimulate insulin secretion, and exert anti-inflammatory effects, 13-OAHSA may play a pivotal role in managing metabolic syndrome and inflammation.

1-Deazaadenosine, an adenosine deaminase inhibitor (Ki: 0.66 μM), may treat cancer, particularly lymphoproliferative disorders.

HSD17B13-IN-3 (compound 2) is a potent inhibitor of hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13), lacking cellular experimental activity [1].

FXIa-IN-7 is an orally available, selective and potent inhibitor of factor XIa for the study of thrombophilia.

ICMT-IN-8 (compound 30) serves as an inhibitor of ICMT, exhibiting an IC50 value of 0.652 μM [1].

VU0155069 hydrochloride (CAY10593 hydrochloride) is a potent and selective inhibitor of phospholipase D (PLD), exhibiting IC50 values of 46 nM for PLD1 and 933 nM for PLD2. It effectively inhibits the migration of both human and mouse breast cancer cell lines [1] [2].

CM-10-18: potent ER α-glucosidase inhibitor, strong antiviral against hemorrhagic fever viruses, protects mice from dengue fatality.

Monohydroxy melphalan, a degradation product and DNA alkylating agent derived from melphalan, results from melphalan hydrolysis in aqueous solutions such as cell culture medium and human plasma. It enhances DNA adducts in ML-1 myeloblastic leukemia cells based on concentration and induces cytotoxicity with an IC50 value of 28.1 μg/ml.

cKK-E15, a peptide-lipid, is instrumental in formulating LNP3 alongside C14PEG2000, unmodified cholesterol, and DOPE [1].

Oseltamivir acid methyl ester, a CES1-convertible neuraminidase inhibitor, serves as an antiviral prodrug.

C12-113, a lipidoid delivery agent, effectively transfects siRNA into cells and, when combined with additional lipids, forms lipid nanoparticles (LNPs). These LNPs facilitate the delivery of mRNA encoding the spike glycoprotein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in mice [1] [2].

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