Metabolismo

<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>CYP17-IN-1 is an effective oral inhibitor of CYP17 that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.</p>

<p>ICMT-IN-38 (Compound 42) is an ICMT inhibitor, demonstrating an IC50 value of 0.049 μM [1].</p>

<p>Yonkenafil, a PDE5 inhibitor, may reduce stroke damage and aid in Alzheimer's treatment.</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>3-Oxo Atorvastatin is an impurity of Atorvastatin. Atorvastatin is an HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.</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>JTT 551: Selective PTP1B inhibitor for type 2 diabetes research; Ki=0.22μM for PTP1B, 9.3μM for TCPTP.</p>

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

<p>Bemoradan is an inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue</p>

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

<p>C18 ((±)-2'-hydroxy) Ceramide (d18:1/18:0) is a lipid molecule that can be used in life science related research. The CAS number of C18 ((±)-2'-hydroxy) Ceramide (d18:1/18:0) is 34249-41-7.</p>

<p>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are recent discoveries in endogenous lipids that are influenced by dietary changes such as fasting and high-fat diets, showing a link with enhanced insulin sensitivity in mice. These compounds typically feature a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) bound to a hydroxy group on another C-16 or C-18 fatty chain. A specific FAHFA, 9-POHSA, consists of palmitoleic acid connected at the hydroxy stearic acid's 9th position. This molecule, in particular, exhibits notably increased levels in the serum of glucose-tolerant AG4OX mice, which express the Glut4 glucose transporter predominantly in their adipose tissue. Given the broader family of FAHFAs' roles in enhancing glucose tolerance, promoting insulin secretion, and exerting anti-inflammatory effects, 9-POHSA emerges as a potential bioactive lipid involved in managing metabolic syndrome and inflammation.</p>

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

secreted phospholipase A2 (sPLA2) inhibitor

<p>BMS-185411 is a bio-active chemical.</p>

<p>HIF-2α-IN-13 (18) acts as a HIF-2α inhibitor and exhibits an IC 50 value of 2.7 μM.</p>

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

<p>h-NTPDase-IN-5 (compound 3b) serves as a pan-inhibitor of NTPDase, exhibiting inhibitory concentration 50 (IC50) values of 1.10 μM (h-NTPDase1), 44.73 μM (h-</p>

<p>Mal-Pc, a maleimide phthalocyanine, depletes GSH to reduce aggregation and boost ROS, improving PDT against cancer.</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>1,2-Dilauroyl-sn-glycero-3-phospho-(2R)-glycerol is a type of phosphoglycerol characterized by the presence of lauric acid at the sn-1 and sn-2 positions. [Matreya, LLC. Catalog No. 1443]</p>

<p>ML395 is a potent, selective PLD2 allosteric inhibitor with potent antiviral activity (IC50 =360 nM).</p>

<p>MS-444 (BE-34776) is an MLCK and HuR inhibitor with antitumor activity that can be used to study triple-negative breast cancer and colorectal cancer.</p>

Fasidotril inhibits NEP/ACE, treats high blood pressure in rats, effective in humans with hypertension.

IDH1 Inhibitor 3 is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor (IC50: 45 nM for IDH1R132H).

<p>1,2-Dilinoleoyl-sn-glycero-3-PC (Dilinoleoyllecithin), a phospholipid, finds application in the production of artificial membranes [1].</p>

<p>MMV009085 is a potent inhibitor of the Plasmodium falciparum hexose transporter (Pf HT1), with potential as an anti-malarial agent.</p>

<p>Magmas-IN-1 (compound 9), a small molecule Magmas inhibitor (SMMI), targets the mitochondria-associated granulocyte-macrophage colony-stimulating factor (GM-CSF</p>

<p>C14-SPM, a branched-chain polyamine lipidoid, facilitates the delivery of siRNA [1].</p>

<p>PPARδ agonist 9 (compound 21), with an EC50 of 3.6 nM, is effective in vivo, decreasing serum MCP-1 concentrations in mice and markedly reducing atherosclerotic</p>

<p>Raloxifene Bismethyl Ether hydrochloride is a Raloxifene metabolite and an estrogen receptor inactive compound on which both hydroxyl groups are absent.</p>

<p>9(Z),11(Z)-Octadecadienoic acid, an isomer of linoleic acid, demonstrates antitumor activity with an EC50 value of 446.1 µM [1].</p>

<p>Perindopril acyl-β-D-glucuronide is a metabolite of the ACE inhibitor perindopril [1].</p>

hCAIX-IN-16 (Compound 12d), an inhibitor of hCA IX, exhibits inhibition constants (K i) of 190.0 nM for hCA IX and 187.9 nM for hCA XII.

<p>ICMT-IN-5 (compound 46) is an ICMT inhibitor with an IC50 value of 0.3 μM [1].</p>

<p>MγLnFP, an analog of methyl arachidonyl fluozophosphonate (MAFP), holds significance in pharmacological research due to its potential as an inhibitor of phospholipases, FAAH, and its role as a CB receptor ligand. However, the properties and effects of the γ-linolenyl variant of MAFP remain to be fully explored.</p>

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

<p>VU0364739, a selective phospholipase D2 (PLD2) inhibitor with an IC50 of 22 nM, effectively reduces cancer cell proliferation [1].</p>

<p>BMS-986172 is an orally active, highly selective inhibitor of MGAT2, demonstrating inhibitory concentrations (IC50) of 4.6 nM for human MGAT2 (hMGAT2) and 20 nM</p>

<p>1-Isopropyltryptophan (1-IsoPT), an IDO1 inhibitor, suppresses the expression of IDO-1 and IDO-2 mRNA induced by IFN-γ stimulation [1].</p>

<p>PHD-IN-1 (compound 80) serves as a potent PHD2 inhibitor, exhibiting an IC50 value of ≤5 nM.</p>

<p>IDO1/TDO-IN-6 (compound 11) is a dual inhibitor targeting IDO1 and TDO, exhibiting IC50 values of 2.25 μM for IDO1 and 2.89 μM for TDO.</p>

<p>ICMT-IN-17 (compound 52) serves as an ICMT inhibitor, exhibiting an IC50 value of 0.38 μM [1].</p>

<p>Quizalofop-P, a selective herbicide, is absorbed by weed stems and leaves before translocating both upward and downward within the plant, concentrating in</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-Acyl taurines, such as N-lignoceroyl taurine, alongside various arachidonoyl amino acid conjugates like N-arachidonoyl dopamine and N-arachidonoyl-L-serine, have been identified in bovine brain and through mass spectrometry lipidomic studies in the brain and spinal cord of both wild-type and FAAH knockout mice. Notably, N-lignoceroyl taurine levels were found to be 23-26 times higher in FAAH knockout mice than in wild types, suggesting its degradation by FAAH, despite in vitro evidence showing FAAH hydrolyzes N-lignoceroyl taurine significantly slower than oleoyl ethanolamide. Additionally, N-acyl taurines with polyunsaturated acyl chains are known to activate TRPV1 and TRPV4 channels within the transient receptor potential (TRP) family of calcium channels.</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>1,2-Dinonadecanoyl-sn-glycero-3-PC (DNPC), a saturated phospholipid, serves as a standard in quantifying phosphatidylcholines in human synovial fluid and has been utilized in researching lipid bilayer phase transition dynamics.</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>