Métabolisme

<p>Lateritin (Bassiatin) is An Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor and a platelet aggregation inhibitor from the mycelial cake of Gibberella</p>

<p>hMAO-B-IN-32 is a potent hMAO-B selective inhibitor with an IC50 of 45.52 μM.</p>

<p>CRX000227 is a PPAR modulator suitable for researching metabolic and cell proliferative disorders [1].</p>

<p>2-Phenyl-2-(2-pyridyl)acetonitrile represents the principal metabolite of the antigastric agent SC 15396, produced by the supernatant fraction of rat liver</p>

<p>4′-DTMP (4-Demethyltrimethoprim) is a DHFR inhibitor with antimicrobial activity against Escherichia coli.</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>

MR-2-93-3, a long-chain fatty acid, functions as a carrier for polynucleotides [1].

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are lipids recently discovered to be modulated by dietary influences such as fasting and high-fat feeding, and they play a role in enhancing insulin sensitivity. These compounds typically feature a carbon-16 or carbon-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) esterified to a carbon-16 or carbon-18 hydroxy fatty acid. A specific example is 12-SAHSA, which consists of stearic acid linked to 12-hydroxy stearic acid. Notably, 12-SAHSA levels are found to be moderately increased in the serum of glucose tolerant AG4OX mice, a model characterized by adipose tissue-specific overexpression of the Glut4 glucose transporter.

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.

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

<p>ICMT-IN-10 (compound 32) serves as an inhibitor for ICMT, exhibiting potent activity with an IC50 value of 0.184 μM [1].</p>

ICMT-IN-11 (compound 48) serves as an ICMT inhibitor with an IC50 value of 0.031 μM [1].

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are recently discovered lipids that play a role in the body's response to fasting and high-fat diets, with a link to insulin sensitivity. These compounds consist of a long-chain fatty acid (such as palmitoleic, palmitic, oleic, or stearic acid) bonded to a hydroxy fatty acid, both ranging in length from C-16 to C-18. Specifically, 12-OAHSA is a type of FAHFA where oleic acid is attached to the 12th carbon of hydroxy stearic acid. Within the FAHFA family, OAHSAs are particularly notable for their high concentration in the serum of AG4OX mice, a strain engineered to express the Glut4 glucose transporter predominantly in their adipose tissue, which demonstrates an enhanced glucose tolerance.

ICMT-IN-24 (compound 63) is an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting potent activity with an IC50 value of 0.19 μM [1].

BML-288 is a phosphodiesterase Type II (PDE2) inhibitor that demonstrates no inhibition of 5-lipoxygenase (5-LO) or cyclooxygenase (COX-1).

<p>1,2-Dioleoyl-3-linoleoyl-rac-glycerol (OOL) is a triglyceride featuring oleic acid at the sn-1 and sn-2 positions and linoleic acid at the sn-3 position. This compound is prevalent in several seed and vegetable oils, such as those from pumpkin seeds, olives, and sesame.</p>

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

1-Myristoyl-2-palmitoyl-3-butyryl-rac-glycerol, a triacylglycerol with myristic acid (at the sn-1 position), palmitic acid (at the sn-2 position), and butyric acid (at the sn-3 position), has been detected in human breast milk.

ICMT-IN-30 (compound 67) is an ICMT inhibitor with an IC50 value of 0.27 μM [1].

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

1,2-Diheptadecanoyl-sn-glycero-3-phosphorylcholine (DHPC) is a derivative of phosphatidylcholine (PC) that exhibits biological activity, functioning as a

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

(R)-Palmitoyl-(2-methyl)ethanolamide (Me-PEA) acts as a competitive inhibitor against [3H]-AEA metabolism, exhibiting a K i value of 6.6 μM [1].

SHP2-IN-20 (compound 193), a potent SHP2 inhibitor, exhibits an IC50 of 3 nM, making it suitable for glioblastoma research [1].

5-Lipoxygenase-In-1 (compound example 4.10) is a 5-Lipoxygenase inhibitor.

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

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

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

EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. EMD638683 R-Form is the R-form of EMD638683.

XL041 (BMS-852927) is an agonist of LXRβ-selective.

<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>

<p>CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3).</p>

G43-C3-TEG is a glycosyl-transferase inhibitor that diminishes biofilm formation by inhibiting the synthesis of extracellular polysaccharides (EPS) [1].

Anticancer agent 122, a potent inhibitor of human lactate dehydrogenase A (h LDHA), exhibits significant anticancer activities, rendering it suitable for use in

<p>CYP11A1-IN-1 (compound 30) is a selective inhibitor of the enzyme CYP11A1, displaying an IC50 ranging from 201-2000 nM.</p>

RORγt agonist 2 is a potent agonist of RORγt.

SREBP/SCAP-IN-2 (compound 13) acts as a selective inhibitor of SREBP/SCAP [1].

ICMT-IN-40 (compound 19) is a potent inhibitor of ICMT, exhibiting an IC50 value of 0.031 μM [1].

ICMT-IN-3 (Compound 27) serves as a potent inhibitor of ICMT, demonstrating an IC50 value of 0.015 μM [1].

<p>"Lipid AX4, characterized as an ionizable cationic lipid with a pKa of 6.89, facilitates the formation of lipid nanoparticles (LNPs) for in vivo mRNA delivery [1]."</p>

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) have emerged as significant regulators of metabolic processes, influenced by dietary changes such as fasting and high-fat diets, and are linked to improved insulin sensitivity in mice. These compounds typically feature a fatty acid chain, either C-16 or C-18 in length (for example, palmitoleic, palmitic, oleic, or stearic acid), esterified to a hydroxy fatty acid of similar length. A specific FAHFA, 12-POHSA, involves the esterification of palmitoleic acid to the 12th carbon of stearic acid. Notably, 12-POHSA levels are markedly higher in the serum of AG4OX mice, which exhibit enhanced glucose tolerance due to overexpression of the Glut4 glucose transporter in adipose tissue. Given the capacity of FAHFAs to enhance glucose tolerance, stimulate insulin secretion, and exert anti-inflammatory actions, 12-POHSA holds potential as a bioactive lipid implicated in managing metabolic syndrome and inflammation.

C24:1 1-Deoxyceramide (m18:1/24:1(15Z)) is a lipid molecule that can be used in life science related research. The CAS number of C24:1 1-Deoxyceramide (m18:1/24:1(15Z)) is 1246298-58-7.

ICMT-IN-32 (compound 70) acts as an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.777 µM [1].

SHP2-IN-17 (compound 192) is a potent inhibitor of SHP2, exhibiting an IC50 of 2 nM and holds potential for use in glioblastoma research [1].

FAAH Inhibitor 2 (Compound 17b) is an irreversible inhibitor of fatty acid amide hydrolase (FAAH), demonstrating an IC50 value of 0.153 μM [1].

CHK-336 (Example 1), an orally active LDHA inhibitor (IC50 <1 nM), suppresses lactate production in mouse hepatocytes and is applicable in hyperoxaluria

<p>ICMT-IN-41 (compound 20) serves as a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.069 μM [1].</p>

5-PAHSA, a FAHFA formed through the formal condensation of the carboxy group of palmitic acid with the hydroxy group of 5-hydroxystearic acid, serves as a human metabolite, possesses anti-inflammatory and hypoglycemic properties, and is categorized as a long-chain fatty acid. This compound, deriving from hexadecanoic acid and octadecanoic acid, is the conjugate acid of a 5-PAHSA(1-).

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