Métabolisme

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are endogenous lipids that are influenced by fasting and high-fat diets and linked to improved insulin sensitivity in mice. These compounds typically feature a chain of either 16 or 18 carbon atoms (for example, palmitoleic, palmitic, oleic, or stearic acid) esterified with a hydroxy fatty acid chain of similar length. One specific FAHFA, known as 5-OAHSA, consists of oleic acid bonded to the fifth carbon of hydroxy stearic acid. Within the FAHFA family, OAHSAs exhibit the highest serum levels in AG4OX mice, which are known for their glucose tolerance attributed to the overexpression of the Glut4 glucose transporter in adipose tissue.

ICMT-IN-23 (compound 36) serves as an inhibitor of ICMT, exhibiting a half-maximal inhibitory concentration (IC50) of 0.123 μM [1].

Cis-13-Octadecenoic acid, a monounsaturated fatty acid, is identified in bovine milk fat.

ATX inhibitor 21 is a potent inhibitor of ATX (IC50: 3490 nM).

2-Myristyldistearin (SMS), a triacylglycerol comprising myristic acid and stearic acid [1], showcases its intricate structural composition.

1a,1b-Dihomo Prostaglandin F2α (1a,1b-dihomo PGF2α), a hypothetical product of adrenic acid in the COX pathway, is predominantly synthesized in the renal medulla, reflecting the selective distribution of adrenic acid in this region.

S-Benzylglutathione acts as a competitive inhibitor of glutathionase and undergoes conversion by rat kidney microsomes into its cysteine derivatives.

Prostaglandin F2α-1-glyceryl ester undergoes oxidation via 15-hydroxyprostaglandin dehydrogenase (15-HPGDH) [1].

BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa; Kis: 0.2 and 0.42 nM for human and rabbit FXIa).

WT IDH1 Inhibitor 2 blocks wild-type and R132H mutant IDH1 (IC50: 120 nM); related to GSK321.

AR453588 hydrochloride is an orally bioavailable anti-diabetic glucokinase activator (EC50: 42 nM) with anti-hyperglycemic activity.

"(±)-2'-Hydroxy Ceramide (d18:0/18:0) is a sphingomyelin derivative isolated from mammalian platelets upon ADP stimulation [1]."

N-Palmitoyl taurine, an amino-acyl endocannabinoid prominent in rat brain lipidomics profiling, accompanies multiple arachidonoyl amino acids isolated from bovine brain, including N-arachidonoylethanolamine (NADA) and N-arachidonoyl serine (ARA-S). Mass spectral lipidomic analysis of rat brain additionally revealed a series of fatty acyl amides with taurine. The function of N-Palmitoyl taurine is under investigation.

ICMT-IN-37 (compound 41) serves as an inhibitor of ICMT with an IC50 value of 0.308 μM [1].

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]

ICMT-IN-33 (compound 73) functions as an ICMT inhibitor with an IC50 value of 0.46 μM [1].

SHP2-IN-19 (compound 183) is a SHP2 inhibitor exhibiting potent activity with an IC50 of 3 nM, and is utilized in glioblastoma research [1].

MSI-1436 is a selective, non-competitive the enzyme protein-tyrosine phosphatase 1B (PTB1B)inhibitor(IC50 of appr 1 μM)

UK 357903, a phosphodiesterase 5A (PDE5A) inhibitor, is used potentially for the treatment of erectile dysfunction.

Lp-PLA2-IN-9, a tetracyclic pyrimidinone, inhibits rhLp-PLA2 (pIC50: 10.1), promising for neurodegenerative research.

<p>15-PGDH-IN-2 (Compound 2) is an inhibitor of 15-PGDH with an IC50 value of 0.274 nM. This compound is useful for research into hair loss, bone formation, gastric ulcer healing, and dermal wound healing [1].</p>

1-Stearoyl-2-hydroxy-sn-glycero-3-PG, a lysophospholipid characterized by the presence of stearic acid (18:0) at the sn-1 position, finds application in the creation of micelles, liposomes, and various artificial membranes, including those utilized in lipid-based drug delivery systems.

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

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

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.

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

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

<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>

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

TMP778 is an effective and selective RORγt inverse agonist (IC50: 7 nM in FRET assay).

ICMT-IN-1 (compound 75) is a potent ICMT inhibitor with an IC50 value of 0.0013 μM.

Tetrahydro-11-dehydrocorticosterone is an inhibitor of 11β-hydroxysteroid dehydrogenase [1].

GLX481304 is a selective Nox-2 and Nox-4 inhibitor, exhibiting IC50 values of 1.25 μM.

Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC50s of 8.092 and 45.320 μM for yeast and human.

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

Iganidipine（NKY 722） is a new water-soluble Ca2+ antagonist with antihypertensive activity for research and neurological related diseases.

MK-8189 is a potent and selective pyrimidine PDE10A inhibitor, with excellent PDE (phosphodiesterase) selectivity for the treatment of schizophrenia.

Quetiapine sulfoxide dihydrochloride, a major metabolite of second-gen antipsychotic Quetiapine, modulates 5-HT and dopamine receptors.

<p>FAS-IN-1 Tosylate is an effective fatty acid synthase inhibitor;Has an IC50 of 10 nM.</p>

Autotaxin-IN-4 is an Autotaxin inhibitor. It has the potential to treat idiopathic pulmonary fibrosis.

<p>Moexiprilat, an active metabolite of the prodrug moexipril formed through side chain ester hydrolysis in vivo, functions as an angiotensin-converting enzyme (</p>

α-Glucosidase-IN-11 is a highly permeable competitive inhibitor of α-glucosidase (IC50: 0.56 μM).

NUCC-0223619 is an IDO1 inhibitor that induces the degradation of IDO protein and can be involved in the synthesis of PROTAC.

DPM-1001 trihydrochloride: Potent PTP1B inhibitor, IC50 100 nM, oral, non-competitive, anti-diabetic.

Compound 22g: potent GLO1 inhibitor; IC50=0.011 μM; potential for depression, anxiety research.

CJ-463, a selective uPA blocker, shows strong anti-tumor effect, especially at 100mg/kg, potentially treating lung cancer.

<p>IDH1 Inhibitor 5 targets MOG cells (IC50: 64.4 nM) and R132H mutant IDH1 gliomas (IC50: 34.9 nM).</p>

SH-BC-893: Oral anti-cancer sphingolipid analog, prevents ceramide-related mitochondrial issues, and tackles diet-related obesity.

DHODH-IN-22: potent, selective DHODH inhibitor, orally active, IC50: 0.3 nM, for AML research.

Mitochondria degrader-1, a potent autophagy inducer, aids in neurodegenerative, cancer, and aging disease research.