Metabolism

3β,7β-Dihydroxy-5-cholestenoic acid is a C27 acid whose levels are elevated in Niemann-Pick Type C and B diseases, leading to toxicity in ocular motor neurons. It is synthesized by the enzymatic action of hydroxysteroid 11-β dehydrogenase 1 from 3β-hydroxy-7-oxocholest-5-en-(25R)26-enoic acid (3βH,7O-CA).

MGAT2-IN-1 is an orally active monoacylglycerol acyltransferase (MGAT2)inhibitor (human and mouse MGAT2 with IC50 of 7.8 and 2.4 nM , respectively).

1,2-Dipentadecanoyl-rac-glycerol (DG(15:0/15:0/0:0)) is a compound referenced in studies examining the effect of insulin on the content of 1,2-diacylglycerol in rat hearts. Insulin is observed to increase the amount of 1,2-diacylglycerol containing specific fatty acid compositions in the heart, which may be linked to cardiac contractility.

RO5101576 is a potent antagonist of LTB4 receptor.

<p>Diacylglycerolacyltransferaseinhibitor-2 (Example 8) acts as an inhibitor for diacylglycerol acyltransferase 2 (DGAT2), exhibiting an IC50 value of 3.7 nM.</p>

<p>MAGL-IN-18 (compound 118) serves as a highly potent inhibitor of Monoacylglycerol lipase (MAGL), demonstrating an IC 50 value of 0.03nM.</p>

Compound 13, identified as h15-LOX-2 inhibitor 3, exhibits inhibitory activity against h15-LOX, with IC50 and Ki values of 25 μM and 15.1 μM, respectively.

SelB-1 acts as a dual inhibitor of Topoisomerase I/II (TopoisomeraseI/II), exhibiting anticancer activity suitable for research on prostate and colon cancers. Additionally, SelB-1 can induce the expression of autophagy (autophagy) genes and lipid peroxidation while reducing GSH levels.

<p>MK-3168 (12C) functions as a FAAH inhibitor, exhibiting IC50 values of 1.0 nM, 5.5 nM, and 1.7 nM for human, rhesus, and rat respectively. It demonstrates effective brain uptake and FAAH-specific signaling. Additionally, 11 C MK-3168 is applicable as a FAAH PET tracer.</p>

α-Glucosylrutin is an effective antioxidant known for its activity in scavenging free radicals. Due to its high epidermal bioavailability, it is commonly utilized in studies related to skin aging.

hCAIX-IN-20 (compound APBS-5m) is a potent inhibitor of carbonic anhydrase IX (hCA IX), with a Ki of 2.7 nM, playing a significant role in cancer research.

Urobilin hydrochloride, a metabolic byproduct of Hemoglobin, is excreted through urine and feces in various mammals. It also serves as an indicator of human waste contamination.

RWJ 22108 is a bronchial-selective calcium channel (calcium channel) blocker that exhibits an IC50 of 5.7 nM in dog bronchial smooth muscle calcium-dependent contractions.

IDO1-IN-25, a dual inhibitor of IDO1/TDO2, showcases IC50 values of 0.17 μM for IDO1 and 3.2 μM for TDO2. It effectively suppresses NO production in RAW264.7 cells following stimulation with lipopolysaccharide (LPS). Additionally, IDO1-IN-25 demonstrates anti-inflammatory properties in a mouse ear edema model of acute inflammation induced by croton oil.

6′SLN is a characteristic glycan found on the surface of cancer-related extracellular vesicles (EVs) and serves as the primary form of protein glycosylation within EVs. Additionally, 6′SLN, a derivative of sialic acid, interacts with hemagglutinins (HAs) from both human and avian influenza strains, making it relevant in the study of anti-influenza drugs.

Compound 3, known as 5-LOX/MAOs-IN-1, acts as an inhibitor of 5-LOX/MAOs and is an effective free radical scavenger, displaying antioxidant characteristics. It has demonstrated neuroprotective effects in cell models damaged by oxidative stress and is capable of activating the neurogenesis microenvironment in adult mouse neural stem cells. This compound is utilized in research focused on neurodegenerative diseases.

3-Oxochenodeoxycholic acid is an endogenous metabolite detectable in feces and may serve as a diagnostic marker for various diseases, including COVID-19.

D-Citrulline (H-D-Cit-OH), a stereoisomer of L-citrulline, effectively reduces cardiac contractile dysfunction caused by polymorphonuclear leukocyte (PMN) in isolated perfused rat hearts undergoing ischemia/reperfusion. This protective effect is mediated through a non-NO-mediated mechanism.

Lipid PPz-2R1 is an ionizable cationic lipid employed in crafting lipid nanoparticles (LNPs) for mRNA delivery both in vitro and in vivo. LNPs with lipid PPz-2R1, encapsulating an mRNA reporter, target the lungs preferentially over the heart, liver, spleen, and kidneys in mice. Additionally, these LNPs, when encapsulating mRNA encoding phosphatase and tensin homolog (PTEN), enhance PTEN protein levels in PTEN-deficient Lewis lung carcinoma (LLC) cells. In an orthotopic murine LLC model, these Lipid PPz-2R1-containing LNPs, carrying PTEN mRNA, reduce tumor growth either when administered alone or alongside an antibody against programmed cell death protein 1 (PD-1).

DDO-3733 is a conformational activator of Protein Phosphatase 5 (PP5) that functions independently of TRP, facilitating the dephosphorylation of downstream substrates.