Metabolismo

α-glucosidase/PTP1B-IN-1 (compound 8a) is an effective inhibitor of both α-glucosidase and PTP1B, with IC50 values of 66.3 μM and 47.0 μM, respectively. It also exhibits strong inhibitory activity against α-amylase, having an IC50 of 30.62 μM. This compound is capable of binding to the active sites of α-glucosidase and PTP1B. α-glucosidase/PTP1B-IN-1 holds potential for reducing postprandial blood glucose levels and may be useful in managing type 2 diabetes.

<p>Xanthine oxidase-IN-16 is an effective orally active inhibitor of xanthine oxidase (XO), demonstrating significant therapeutic efficacy in rats with hyperuricemia and an IC50 of 102 nM.</p>

SR-4995 (CID 16016685) is an ABHD5 ligand, directly binding to ABHD5 and stimulating lipolysis by releasing it from PLIN.

(24R)-MC 976 is a derivative of Vitamin D3.

<p>1-Naphthyl 3,5-dinitrobenzoate (JMC-4) is an inhibitor of 5-LOX can be used in studies about inflammatory therapy.</p>

<p>Cholesteryl homo-γ-linolenate is a cholesterol ester.</p>

<p>SX29 is a non-competitive α-glucosidase inhibitor with oral activity, exhibiting an IC50 of 2.12 μM. It possesses hypoglycemic properties; oral administration of SX29 reduces blood glucose levels and enhances glucose tolerance in diabetic mice.</p>

<p>α-Glucosidase-IN-74, a nicotinamide-thiazole derivative, functions as an α-glucosidase (α-glucosidase) inhibitor. It demonstrates antidiabetic activity by reducing blood glucose and triglyceride levels in Streptozotocin-induced diabetic animals.</p>

O-desmethyl Mebeverine acid is a metabolite of Mebeverine.

NIM811 is an orally bioavailable dual inhibitor of mitochondrial permeability transition and cyclophilin.

<p>ω-Conotoxin Bu8 is a 25-amino-acid-residue ω-conotoxin that features three disulfide bridges.</p>

DSPE-PEG5000-NYZL1 is a PEG compound composed of DSPE and NYZL1, where NYZL1 specifically binds to bladder cancer tissues and cells. DSPE-PEG5000-NYZL1 is applicable for drug delivery.

PK-10, when combined with Fluconazole, exhibits potent synergistic antifungal activity against multiple Fluconazole-resistant Candida albicans strains.

Leucylproline is a peptide that proteolytic breakdown product by larger proteins.

<p>Pectin, a plant cell wall derived heteropolysaccharide, forms nanoparticles for delivery and acts as an antimicrobial adsorbent.</p>

CstII (ST8Sia VI), an alpha-2,8-sialyltransferase, catalyzes α2,8 oligo/polysialic acid chain elongation. Used in biochemical research.

<p>SF2312 ammonium is the ammonium salt of SF2312, a phosphonate antibiotic and enolase inhibitor derived from the actinomycete Micromonospora and active under</p>

SHP2-D26: potent SHP2 degrader binding VHL-1/SHP2, neddylation & proteasome-dependent.

Myristoyl coenzyme A lithium, a compound marked by lithium in its myristoylated form, plays a crucial role in the biochemical mechanism of myristoylation, essential for both viral functionalities and tumor growth in colon epithelial cells. This process is predominantly governed by N-myristoyltransferase (NMT), which exhibits increased activity in colon epithelial tumors compared to normal cells. The activity of NMT is significantly influenced by the reduction of coenzyme A (CoA), a vital regulator that enhances NMT's ability to induce myristoylation, unlike its oxidized form which impedes this process. Consequently, Myristoyl coenzyme A serves as an inhibitor to the demyristoylation activity, showcasing its potential as an anticancer and antiviral agent.

Methyl ester of 11(Z),14(Z)-eicosadienoic acid is a ω-6 PUFA, inhibits LTB4 binding and IMP dehydrogenase, and might affect sleep.

S32826, a potent autotaxin inhibitor with an IC50 of 8.8 nM, blocks LPA release and targets α, β, γ isoforms.

<p>Z-Asp(OBzl)-OH (N-Cbz-L-Aspartic acid 4-benzyl ester) is an aspartic acid derivative.</p>

<p>α-Glucosidase-IN-27 (compound 8l), an α-glucosidase inhibitor with an IC50 value of 25.78 μM, demonstrates potential for research into type 2 diabetes (D2M) [1</p>

<p>GLUT1-IN-1 inhibits GLUT1; cytotoxic to HeLa, A549, HepG2 (IC50: 5.49, 11.14, 8.73 μM); potential in PDT and cancer research.</p>

<p>Fmoc-Tyr(3-F,tBu)-OH: Cyclic peptide with high permeability, target-specific affinity. Sourced from WO2018225864A1.</p>

<p>2,6-Diphenylpyridine is toxic to MDA-MB-231 cells and has anticancer potential.</p>

<p>hBChE-IN-4 (compound 40) serves as an effective activator for hCA and an inhibitor for BChE. It demonstrates affinity for various hCA subtypes with affinity constants (KA) of 266 nM for hCA I, 76.9 nM for hCA II, 918 nM for hCA IV, 893 nM for hCA VB, and 98.0 nM for hCA VII. Inhibition concentrations (IC50) for eeAChE and eqBChE are recorded at 72.1 nM and 4.2 nM, respectively. hBChE-IN-4 is non-cytotoxic and has demonstrated potential cognitive enhancement effects. It holds potential for research in neurodegenerative and other neuropsychiatric disorders.</p>

Cytochrome P450 metabolism of polyunsaturated fatty acids produces numerous bioactive epoxide regioisomers.

<p>Netupitant N-oxide is a highly selective antagonist of NK1 receptor, is Netupitant metabolite.</p>

Compound PDK0326, with CAS No. 6631-94-3, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound PDK0326 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

<p>KKII5 is a potent inhibitor of the lipoxygenase LOX-1 with an IC50 of 19 μM.KKII5 inhibits lipid peroxidation and enhances the ability of the active centers of</p>

<p>2-Methoxy-4-propylphenol is an inhibitor of human carbonic anhydrase isoenzymes 1/2/9/12 and has antifungal activity.</p>

<p>BMT-297376, the optimized Linrodostat, is a potent IDO1 inhibitor.</p>

<p>Streptolysin O: lyses cells, cardiotoxic, used for cell permeabilization, has active and inactive states.</p>

Ribulose: key in pentose metabolism, aids L-ribose isomerase study, yeast engineering, and chiral compound research.

DSPE-PEG2000-TAT is a PEG compound consisting of DSPE and the cell-penetrating peptide (TAT) peptide. It can be used for drug delivery.

<p>γ-Glu-Gly TFA, a γ-glutamyl dipeptide, is a human lipid metabolite with a structure resembling GABA (γ-aminobutyric acid).</p>

<p>Trimipramine N-oxide, a trimipramine metabolite, inhibits hNAT, hSERT, hDAT, and hOCT1/2 with IC50s 11.7-27.4 nM; for depression/anxiety research.</p>

<p>α-Glucosidase-IN-89 (8g) is an inhibitor of α-glucosidase, with an IC50 of 0.5 μM and a Ki of 0.46 μM.</p>

trans-2-Hexadecenoyl-L-carnitine is an endogenous metabolite in urine[1].

<p>IDO1/TDO-IN-7 (Compound 43b), an isochinoline derivative, functions as a potent dual inhibitor of IDO1/TDO with IC50 values of 0.31 μM and 0.08 μM, respectively. Demonstrating favorable pharmacokinetics and strong antitumor efficacy in the B16-F10 tumor model, this compound also exhibits low toxicity.</p>

<p>WH-15: fluorogenic reporter for PLC-γ1, PLC-δ1, PLC-β2 with Km values of 49; 30, 86.1 µM. Cleaves to fluorescent 6-aminoquinoline for live cell imaging.</p>

<p>Anti-osteoporosis agent-10 is an inhibitor of osteoporosis that suppresses the formation of osteoclasts with an IC50 of 0.042 μM. It also exhibits antagonistic activity towards PPARγ, with an EC50 value of 0.75 μM.</p>

<p>9(R)-HODE cholesteryl ester, from atherosclerotic lesions, may form enzymatically or by lipid peroxidation; used as a chiral analysis standard.</p>

<p>Omfiloctocog alfa (SCT-800) is a recombinant FVIII for Hemophilia A research.</p>

Fmoc-Phe(4-NH2)-OH (Fmoc-4-Amino-L-phenylalanine) is a phenylalanine derivative used in research on supramolecular hydrogels.

<p>5MPN is a PFKFB4 inhibitor that inhibits the F6P binding site and suppresses the proliferation of myeloma cells.</p>

<p>Lysine-N,N-diacetic acid (BCML) is a highly efficient TAS2R4 inhibitor, blocking the human TAS2R4-mediated response to quinine.</p>

<p>Compound Fr14500 is a natural product for research related to life sciences. The catalog number is Fr14500 and the CAS number is 14667-55-1.</p>

Ezetimibe phenoxy glucuronide (Ezetimibe glucuronide) is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity.