Metabolism

<p>Sampatrilat, an oral vasopeptidase inhibitor, more potently blocks C-domain ACE (Ki=13.8 nM) over N-domain (Ki=171.9 nM).</p>

<p>Temocaprilat (RS5139) is an Angiotensin-converting Enzyme (ACE) inhibitor.</p>

<p>Potent LXR agonist; AC50: 1.5 nM (LXR-α), 12 nM (LXR-β); potential in atherosclerosis research.</p>

<p>RXPA 380: C-terminal ACE inhibitor, Ki=3nM; IC50=2.5nM for C-domain ACE mutants.</p>

<p>Aladotrilat is an inhibitor of neutral endopeptidase. Its prodrug is aladrotril.</p>

<p>Tiracizine HCl, a new class I antiarrhythmic drug, was studied in patients with ischemic heart disease and shown to decrease myocardial contractile function.</p>

<p>Enpp-1-IN-4: potent enpp-1 inhibitor with potential in cancer research. See patent WO2019177971A1, compound 1.</p>

<p>ICMT-IN-2 (compound 45) serves as an ICMT inhibitor with an IC50 value of 0.168 μM [1].</p>

<p>DPM-1001 is an orally bioavailable and non-competitive protein-tyrosine phosphatase (PTP1B) inhibitor (IC50: 100 nM) with the anti-diabetic property.</p>

<p>CKD-519: A CETP inhibitor with an IC50 of 2.3 nM, blocking cholesteryl ester transfer in serum.</p>

<p>NTE-122 is a competitive Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor.</p>

<p>VT-1598 tosylate is a selective, orally active antifungal compound that targets CYP51. It demonstrates efficacy against C. auris.</p>

<p>YM17E is an inhibitor of ACAT with IC50 of 44 nM in rabbit liver microsomes in vitro.</p>

<p>Implitapide Racemate is the racemate of Implitapide. Implitapide is an inhibitor of microsomal triglyceride transfer protein (MTP).</p>

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

<p>"113-O12B is an ionizable cationic lipidoid containing a disulfide bond, utilized in the generation of lipid nanoparticles (LNPs) for mRNA delivery [1]."</p>

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

<p>ERX-41 is an orally active, stereospecific small molecule that targets lysosomal acid lipase A (LIPA).</p>

<p>ICMT-IN-12 (compound 78) serves as an ICMT inhibitor, demonstrating an IC50 value of 0.42 μM [1].</p>

<p>PF-915275 inhibits 11βHSD1 in humans (Ki=2.3 nM, EC50=15 nM) and affects cortisone-cortisol conversion in hepatocytes.</p>

<p>C24:1 dihydro 1-Deoxyceramide (m18:0/24:1) is a lipid molecule that can be used in life science related research. The CAS number of C24:1 dihydro 1-Deoxyceramide (m18:0/24:1) is 1246298-60-1.</p>

<p>RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells),</p>

<p>3-Aminoisobutyric acid, a non-protein amino acid resultant from thymine catabolism, plays a significant role in metabolic activities. At a 5 µM concentration, it triggers browning in primary adipocytes, notably elevating uncoupling protein 1 (UCP-1) and CIDEA expression. Additionally, it boosts PPARα expression in both primary adipocytes and mouse inguinal white adipose tissue (WAT) in vivo, alongside enhancing β-oxidation in hepatocytes. Its plasma levels surge post-exercise in mice, and its administration at 100 mg/kg daily curtails weight gain and body fat without diminishing food consumption or hiking energy output, whilst ameliorating glucose tolerance. Notably, 3-aminoisobutyric acid concentrations are heightened in individuals with β-ureidopropionase deficiency, a genetic flaw impairing pyrimidine degradation, affecting plasma, urine, and cerebrospinal fluid.</p>

<p>Potent CETP inhibitor, boosts HDL-C levels, orally active; IC50=4nM.</p>

<p>BIO-32546 (S-isomer) is a highly potent regulator of autotaxin (ATX) with an IC50 value of 1 nM.</p>

<p>244cis, an ionizable cationic lipid incorporating a piperazine structure, facilitates the creation of lipid nanoparticles (LNPs). These LNPs, when formulated with 244cis and coated with an mRNA reporter gene, exhibit preferential accumulation in the lungs of mice, in contrast to those formulated with SM-102. Additionally, it leads to a reduction in the levels of serum chemokine (C-C motif) ligand 2 (CCL2) [1].</p>

<p>12,15-Epoxy-13-methyl-12,14-eicosadienoic acid, a furan fatty acid first identified in northern pike (E. lucius), exhibits elevated levels in the liver of starving cod.</p>

<p>Z-Pro-Pro-CHO acts as a prolyl oligopeptidase inhibitor with half-maximal inhibitory concentrations (IC50) of 0.16 μM for human prolyl oligopeptidase and 0.01</p>

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

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

<p>GSK2973980A is a selective Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitor (IC50: 3 nM).</p>

<p>Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects.</p>

<p>Bemfivastatin hemicalcium (PPD 10558), an orally active HMG-CoA reductase inhibitor, serves as a lipid-lowering agent.</p>

<p>Lignoceroyl ethanolamide, a fatty N-acyl ethanolamine within the endocannabinoid family, is derived from lignoceric acid, which is found in relatively high concentrations in rat cerebrospinal fluid. However, the specific function and significance of this metabolite remain unclear.</p>

<p>PDP-EA is an activator of fatty acid amide hydrolase(FAAH) and enhances the amidohydrolase activity of FAAH.</p>

<p>1,2-Dimyristoyl-3-palmitoyl-rac-glycerol (MMP) is a triacylglycerol comprising myristic acid and palmitic acid [1].</p>

<p>ICMT-IN-49 (Compound 2) acts as an ICMT inhibitor with an IC50 value of 0.12 μM [1].</p>

<p>C82 acts as an inhibitor of Mycobacterium tuberculosis (Mtb) cyclic dinucleotide phosphodiesterase (CdnP), with an IC50 value of 17.5 µM. This particular enzyme is responsible for breaking down cyclic di-AMP (c-di-AMP) into adenosine 5'-monophosphate (AMP). Notably, C82 demonstrates selectivity for Mtb CdnP over other bacterial cyclic dinucleotide phosphodiesterases (CDN PDEs) such as Yybt, RocR, and Group B Streptococcus (GBS) CdnP, as well as the mammalian CDN PDE ENPP1, and the viral CDN PDE poxin, showing effectiveness at a concentration of 200 µM.</p>

<p>ICMT-IN-20 (compound 54) serves as an ICMT inhibitor with an IC50 value of 0.682 μM [1].</p>

<p>ZK824859 is an oral uPA inhibitor with IC50s: 79 nM (uPA), 1580 nM (tPA), 1330 nM (plasmin).</p>

<p>PDE5-IN-42 is a selective inhibitor of second-generation phosphodiesterase type 5 (PDE5).</p>

<p>Autotaxin-IN-5 is an Autotaxin inhibitor. It has the potential to treat idiopathic pulmonary fibrosis.</p>

<p>Glucosamine Cholesterol, also known as N-Cholesteryl succinyl glucosamine, is a lipid conjugate derived from glucosamine. It plays a crucial role in the development of lipid nanoparticles (LNPs) [1].</p>

<p>ICMT-IN-28 (compound 65) serves as an inhibitor of ICMT, exhibiting significant potency with an IC50 value of 0.008 μM [1].</p>

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

<p>1-Palmitoyl-3-stearoyl-rac-glycerol, a diacylglycerol, features palmitic acid at the sn-1 position and stearic acid at the sn-3 position. This compound appears in palm-based diacylglycerols derived from palm stearin, palm mid fraction, palm oil, and palm olein, as well as in extracts of wheat bran and brewer's spent grain.</p>

<p>PPAR agonist 1 is an agonist of PPAR α/γ, used for reducing blood glucose, lipid levels, reducing body weight, and lowering cholesterol.</p>

<p>Fatty acid amide hydrolase (FAAH), an enzyme responsible for the hydrolysis and inactivation of fatty acid amides like anandamide and oleamide, has been identified as a target by the potent FAAH inhibitor PHOP. PHOP demonstrates remarkable inhibitory activity with K_i values as low as 0.094 nM for human FAAH and 0.2 nM for rat FAAH. Additionally, through a proteomics assay focusing on the serine hydrolase enzyme family, to which FAAH belongs, PHOP's selectivity was evaluated, presenting IC_50 values of 1.1 nM against FAAH, 1.4 nM against triacylglycerol hydrolase (TGH), and greater than 100 µM against an uncharacterized hydrolase (KIAA1363). This specificity profile of PHOP underscores its potential for yielding precise outcomes in studies involving complex biological systems.</p>

<p>GPX4-IN-2 is a potent inhibitor of GPX4, exhibiting antiproliferative activity. It holds potential for cancer research applications.</p>

<p>KH064 is a sPLA2-IIA inhibitor of oral activity.</p>