Metabolismo

<p>Yonkenafil, a PDE5 inhibitor, may reduce stroke damage and aid in Alzheimer's treatment.</p>

<p>N-Arachidonoyl dopamine (NADA) and N-Arachidonoyl serine (ARA-S), among various arachidonoyl amino acids, have been extracted from bovine brain, while a novel series of fatty acyl amides of taurine were unearthed in rat brain through mass spectral lipidomic analysis, indicating the discovery of a new class of compounds also located in the kidney. These compounds are known to activate members of the transient receptor potential (TRP) family of calcium channels. Notably, N-Stearoyl taurine emerges as a significant amino-acyl endocannabinoid identified in rat brain lipidomics profiling.</p>

<p>ICMT-IN-39, also known as compound 18, functions as an inhibitor of ICMT with an IC50 value of 0.031 µM [1].</p>

<p>OSMI-2 is a cell-permeable inhibitor of O-linked N-acetylglucosamine transferase (OGT).</p>

<p>Lp-PLA2-IN-2 is a selective and potent lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2.</p>

<p>DLPA is a phosphatidic acid (PA) that incorporates the medium-chain lauric acid (12:0).</p>

EMT inhibitor-2 blocks CYP3A4 and CYP2C9 (IC50: 49.72, 5.54 μM) and prevents IL-1β/TGF-β-induced EMT.

PDE1-IN-2 is an PDE1 inhibitor(PDE1C, PDE1B and PDE1A with IC50 values of 6, 140 and 164 nM, respectvely).

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

<p>1-Palmitoyl-2-lauroyl-sn-glycero-3-PC (1,2-PLPC) is a phospholipid with palmitoyl (16:0) and lauryl (12:0) acyl chains at the sn-1 and sn-2 positions, respectively. This mixed-chain phosphatidylcholine aids in researching the role of chain-chain contact interactions in maintaining the structural stability of lipid membrane bilayers.</p>

<p>1,2-Dipropionyl-sn-glycero-3-phosphocholine (PC) is a phospholipid characterized by the presence of propionic acid at its sn-1 and sn-2 positions. This compound has applications in the investigation of interactions between water and the phosphocholine headgroup in aqueous solutions.</p>

<p>HSD17B13-IN-2 (compound 1) serves as a potent inhibitor of hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) with demonstrable activity in cellular experiments [1</p>

<p>C16 1-Deoxyceramide (m18:1/16:0) is a lipid molecule that can be used in life science related research. The CAS number of C16 1-Deoxyceramide (m18:1/16:0) is 1246298-56-5.</p>

<p>Homonojirimycin is an alpha-glucosidase inhibitor.</p>

<p>ICMT-IN-13 (compound 49) functions as an inhibitor of ICMT, exhibiting an IC50 value of 0.47 μM [1].</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>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are a class of endogenous lipids whose levels are modulated by fasting and high-fat diets and are linked to insulin sensitivity. These compounds typically consist of a C-16 or C-18 fatty acid, such as palmitoleic, palmitic, oleic, or stearic acid, esterified to a hydroxylated C-16 or C-18 lipid. One specific form of FAHFA, known as 9-OAHSA, involves the esterification of oleic acid to 9-hydroxy stearic acid. Within the FAHFA family, OAHSAs notably represent the predominant form found in the serum of glucose-tolerant AG4OX mice, which uniquely overexpress the Glut4 glucose transporter in adipose tissue.</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>

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

<p>ICMT-IN-9 (compound 47) is a potent ICMT inhibitor with an IC50 value of 0.16 μM [1].</p>

<p>Thioquinapiperifil is a type of phosphodiesterase-5 (PDE-5) inhibitor found in dietary supplements.</p>

<p>JW 618 is a selective inhibitor of ABHD6, demonstrating inhibition concentrations (IC50 values) of 38 nM for mouse ABHD6 and 13 nM for rat ABHD6, indicating its potent activity across species [1].</p>

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

<p>1,2-Dioleoyl-3-stearoyl-rac-glycerol, a triacylglycerol, features oleic acid at the sn-1 and sn-2 positions and stearic acid at the sn-3 position. This compound is present in sunflower, corn, and soybean oils, as well as in ostrich oil.</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>

<p>Monoacylglycerol lipase inhibitor 1, also known as compound 13 [1], is a potent inhibitor of monoacylglycerol lipase.</p>

KCL-286 is an available and potent retinoic acid receptor beta agonist for the amelioration of spinal cord injury (SCI).

<p>GSK356278: selective PDE4A/B/D inhibitor, pIC50~8.7, anti-inflammatory, anxiolytic, cognition-enhancing.</p>

<p>Gisadenafil (UK-369003) is a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM and prevents degradation of cGMP.</p>

<p>(S)-(-)-Bay-K-8644 ((S)-(-)-Bay K 8644) is an agonist of L-type Ca2+ channel and activates Ba2+ currents with an EC50 of 32 nM.</p>

<p>PDE5-IN-2 is a potent, highly selective, and orally active inhibitor of PDE5(IC50 of 0.31 nM)</p>

TMP780 is an inverse RORγt agonist (IC50: 13 nM). RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.

<p>GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM).</p>

<p>Leramistat is a mitochondrial complex I (NIC1) inhibitor that alters cellular metabolism and reduces proliferation in human primary lung fibroblasts.</p>

<p>(R)-Azasetron besylate (SENS-401), an orally active calcineurin inhibitor, has been shown to mitigate cisplatin-induced hearing loss and cochlear damage [1][2].</p>

<p>VULM 1457 is a potent ACAT inhibitor.</p>

<p>HIF-2α-IN-9 (compound 35r) serves as an HIF-2α inhibitor, effectively suppressing VEGF-A with an IC50 of 305 nM, and modulating growth-promoting genes within</p>

<p>Lp-PLA2-IN-14 (Compound 19), an inhibitor of rhLp-PLA2, exhibits a potent inhibitory effect with a pIC50 value of 8.4.</p>

<p>RORγt inverse agonist 14 (8e) is a potent, selective, and orally active compound with an EC50 of 2.5 nM, exhibiting anti-inflammatory activity.</p>

<p>JP104 is an aryl carbamate that irreversibly inhibits fatty acid amide hydrolase (FAAH) with a pIC50 value of approximately 8 [1].</p>

<p>CA Inhibitor 12 strongly blocks CA II (K_i 1.72 nM), also inhibits CA I (271 nM), shows anticancer effects.</p>

<p>PHD2-IN-1, a potent and orally active HIF prolyl hydroxylase 2 (PHD2) inhibitor, exhibits an IC50 of 22.53 nM and is applicable in anemia research [1].</p>

<p>5J-4 is a potent a blocker of calcium release-activated calcium (CRAC) channel and store-operated calcium entry (SOCE).</p>

<p>GPX4-IN-4 (Compound 24) serves as a potent inhibitor of GPX4, applicable in cancer research [1].</p>

<p>LX-1031 is an effective inhibitor of tryptophan 5-hydroxylase. LX-1031 decreases serotonin (5-HT) synthesis peripherally.</p>

FM26, an isoxazole-based RORγt inverse agonist, cuts EL4 IL-17a mRNA; potent with 264 nM IC50.

<p>UK-157147 is a substrate for UGT1A1(Km: 105 μM).</p>

RP 70676 is a potent ACAT inhibitor(rat and rabbit ACAT with IC50 of 25 and 44 nM ).

<p>Entacapone acid (AG 1290) is a selective and reversible inhibitor of catechol-O-methyltransferase(COMT).</p>

<p>3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) (Dehydrolithocholic acid) is a bile acid metabolite and inhibits the differentiation of TH17 cells by directly</p>