Metabolismo

<p>Darodipine (PY-108068) is a dihydropyridine type Ca+2 antagonist.</p>

<p>Nampt-IN-10 TFA, a NAMPT inhibitor, shows potency in A2780 (IC50: 5 nM) and CORL23 (IC50: 19 nM), suitable for ADC payloads.</p>

<p>Pentadecanoyl ethanolamide, a derivative of the endogenous lipid amides (N-acylethanolamines), demonstrates anticonvulsant efficacy in electroshock-induced seizures in mice, exhibiting minimal toxicity [1].</p>

<p>ICMT-IN-43 (compound 22) acts as a potent inhibitor of the enzyme ICMT, exhibiting an inhibitory concentration (IC50) value of 0.04 μM [1].</p>

<p>NC1 is a potent allosteric inhibitor of lymphoid-specific PTPN22, a protein tyrosine phosphatase.</p>

<p>CETP-IN-3 is an inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP.</p>

<p>AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= &gt;10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg/kg.</p>

<p>AZD1092 is the glucokinase enzyme activator.</p>

<p>Glycolithocholic acid (Lithocholic acid glycine conjugate) is a glycine conjugate of lithocholic acid.</p>

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

<p>LB-60-OF61 is a NAMPT inhibitor, a NAMPT inhibitor that displays antiproliferative activity against MYC oncogene-dependent cancer cell lines.</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>Prostaglandin B2 is a dehydration product of PGE2/PGA2 with weak TP receptor activity, raising rabbit pulmonary pressure at &gt;5 ug/kg.</p>

<p>Chinese gallotannin, a non-specific promiscuous inhibitor of α-amylase, exhibits a K(i) value of 0.82 μg/mL against human salivary α-amylase and shows potential</p>

<p>Niraxostat (Y-700) is one of the isocytosine derivatives as xanthine oxidase inhibitors.</p>

<p>CL4H6, a pH-sensitive cationic lipid, serves as the primary constituent of lipid nanoparticles (LNPs). These LNPs are instrumental in targeting and delivering siRNA, leading to a potent gene-silencing response [1] [2].</p>

<p>Adibendan (Adibendanum) is a selective inhibitor of PDE3 with an IC50 of 2.0 μM.</p>

<p>hCAIX-IN-15 is a potent inhibitor of human carbonic anhydrase IX (hCA IX) with an inhibition constant (Ki) of 38.8 nM, exhibiting broad-spectrum anticancer</p>

<p>CYP3A4-IN-2, a potent CYP3A4 inhibitor (IC50: 0.055 μM), is a hydrophobic ritonavir analog with immunosuppressive and antiviral properties.</p>

<p>ICMT-IN-16 (compound 33) functions as an inhibitor of ICMT, demonstrating inhibitory concentration 50% (IC50) efficacy at 0.131 μM [1].</p>

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

<p>CAY10502 inhibits cPLA2α (85 kDa), crucial in inflammation/arachidonic cascade, with 4.3 nM IC50, reducing arachidonic acid in human platelets.</p>

<p>cis-ent-Tadalafil (cis-ent-IC-351) is a potent and selective PDE5 inhibitor that lowers blood pressure.</p>

<p>Me-Indoxam is an inhibitor of sPLA2. It has no effect on arachidonic acid release and platelet activating factor synthesis.</p>

<p>PHD-IN-2 (Compound 91), a potent PHD antagonist with an IC50 of less than 5 nM, effectively stimulates erythropoietin synthesis in HEP3B cells with an EC50 of</p>

<p>FABP4/5-IN-4 (compound E1) effectively inhibits FABP 4 and FABP 5, displaying IC50 values of 3.78 μM and 5.72 μM, respectively. It is significant in the management of metabolic disorders such as diabetes mellitus [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>Tisolagiline (KDS2010) is a potent, highly selective and reversible MAO-B inhibitor oral activity for the treatment of Alzheimer's disease and obesity.</p>

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

<p>Ilepatril, also known as AVE-7688, is a vasopeptidase inhibitor for the treatment of hypertension.</p>

<p>CAY10435, a β-ketooxazapyridine and selective FAAH inhibitor, exhibits antimicrobial properties. It binds non-competitively to the FAAH of Dictyostelium discoideum, demonstrating a Kd value of 0.57 nM [1] [2].</p>

<p>Sch59498 is a potent phosphodiesterase 1c (Pde1c) inhibitor.</p>

<p>ZK824190: oral uPA inhibitor, IC50 - uPA 237 nM, tPA 1600 nM, Plasmin 1850 nM.</p>

<p>L-869298 is a potent and selective inhibitor of PDE4.</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>BMS-262084 is a potent selective β-lactam trypsin inhibitor with therapeutic potential in the treatment of asthma.</p>

<p>Brodimoprim is an inhibitor of dihydrofolate reductase(DHFR).</p>

<p>Pactimibe is a ACAT inhibitor. It has anti-atherosclerotic activity.</p>

<p>9(Z),11(E),13(Z)-Octadecatrienoic acid methyl ester, an isomer of 9(Z),11(E),13(E)-octadecatrienoic acid methyl ester and the methyl ester derivative of 9(Z),11(E),13(Z)-octadecatrienoic acid, serves as a standard for quantifying 9(Z),11(E),13(Z)-octadecatrienoic acid in wild growing pomegranate (P. granatum) seed oil [Matreya, LLC. Catalog No. 1240].</p>

<p>Palmitoleic acid, an ω-7 monounsaturated fatty acid found in macadamia and sea buckthorn oils, enhances both basal and insulin-stimulated glucose uptake, as well as Glut4 protein levels in 3T3-L1 adipocytes at a 200 µM concentration. Ex vivo, at a dosage of 300 mg/kg per day, it significantly increases glucose uptake and both aerobic and anaerobic glycolysis, while decreasing de novo fatty acid synthesis and the activity of lipogenic enzymes, specifically ATP citrate lyase (ACL) and glucose-6-phosphate dehydrogenase (G6PDH), in isolated murine adipocytes. Furthermore, the dietary administration of palmitoleic acid at 300 mg/kg mitigates high-fat diet-induced insulin resistance and liver inflammation in mice.</p>

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

<p>AA 863 is a 5-lipoxygenase inhibitor, it inhibits the proliferation of human glioma cell lines in dose-dependent.</p>

<p>Efipladib is a phospholipase inhibitor. Efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid.</p>

15-PGDH-IN-1: potent oral 15-PGDH inhibitor, IC50=3nM, useful for tissue repair research.

<p>DGAT1-IN-1 is a potent inhibitor of diacylglycerol O- acyltransferase type 1(DGAT1, IC50 of &lt; 10 nM).</p>

<p>PDE12-IN-3 is an inhibitor of phosphodiesterase 12 (PDE12) (pXC50 of 7.68),with antiviral activity.</p>

<p>ICMT-IN-47 (compound 26) acts as an ICMT inhibitor with an IC50 value of 0.76 μM [1].</p>

<p>Compound 1e, also known as ALP/Carbonic anhydrase-IN-1, is a dual inhibitor targeting both carbonic anhydrase (CA) isozymes II, IX, and XII, as well as alkaline</p>

<p>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].</p>

<p>Antiviral agent 46, also known as compound 4, is a cannabidiol (CBD) derivative exhibiting anti-SARS-CoV-2 activity (IC50: 1.90 μM) and ACE2 inhibition (IC50: 1.37 μM) [1].</p>