Metabolism

<p>10,11-Dihydrocarbamazepine (Dihydrocarbamazepine) is used as pharmaceutical intermediates.</p>

<p>JZP-430 is an effective, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) (IC50: 44 nM).</p>

<p>SGN-2FF is an oral fucosyltransferase inhibitor with antitumor activity.</p>

<p>Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) effectively inhibits HIF, has antioxidation, anti-inflammation, and anti-tumor effects.</p>

<p>Zatolmilast (BPN14770) is an allosteric inhibitor of selective phosphodiesterase 4D (PDE4D; IC50s: 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3).</p>

<p>NSP-805 is a potent and selective guinea pig cardiac phosphodiesterase 3 (PDE3) inhibitor.</p>

<p>WAY-640509 is a glucocerebrosidase inhibitor.</p>

<p>NE 10790, similar to risedronate, is a mild bone resorption inhibitor but poorly blocks FPP synthase.</p>

<p>5-R-Rivaroxaban is the (R)-enantiomer of Rivaroxaban, a potent FXa inhibitor with IC50 0.7 nM and Ki 0.4 nM.</p>

<p>LY 195448 (4-(3-(2-Hydroxy-2-phenyl)ethylamino-3-methylbutyl)benzamide) shows antitumor activity in a mouse tumor model, blocking cells in the mid-stage.</p>

<p>Chlormethiazole hydrochloride is an anticonvulsant and sedative. It also has neuroprotective.</p>

<p>SCD1 inhibitor-4 is stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes.</p>

<p>Lunularic acid, a dihydrostilbene analog, efficiently inhibits hyaluronidase activity and can be used as an endogenous growth inhibitor in moss plants.</p>

<p>KPLH1130, a PDK inhibitor, boosts glucose tolerance and reduces inflammation in high-fat diet mice.</p>

<p>XEN723 is a potent thiazolylimidazolidinone Stearoyl-CoA Desaturase (SCD1) inhibitor(IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively).</p>

<p>Ezetimibe inhibits NPC1L1, activates Nrf2, and reduces cholesterol absorption; ent-Ezetimibe is its RRS-enantiomer.</p>

<p>FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) is a potent inhibitor of FAAH(fatty acid amide hydrolase).</p>

<p>Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.</p>

<p>Clevidipine (Clevidipine butyrate) is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood</p>

<p>MF-438 is an effective and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor (EC50: 2.3 nM for rSCD1).</p>

<p>Mifobate (SR-202) 是一种有效且特异性的 PPARγ拮抗剂，可选择性抑制噻唑烷二酮 (TZD) 诱导的 PPARγ 转录活性，IC50为140 μM，具有抗肥胖和抗糖尿病作用。</p>

<p>Amlodipine (UK-48340) is a synthetic dihydropyridine and a calcium channel blocker with antihypertensive and antianginal properties.</p>

<p>Mutant IDH1 inhibitor is an effective inhibitor of mutant IDH1 R132H (IC50: &lt; 72 nM).</p>

<p>Meclofenoxate HCl (Lucidril) boosts memory and cognition; it's a DIMETHYLAMINOETHANOL and p-chlorophenoxyacetic acid ester.</p>

<p>Enarodustat (JTZ-951) is an orally active factor inhibitor of prolyl hydroxylase (EC50: 0.22 μM) and has the potential for renal anemia treatment.</p>

<p>GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) (IC50s: 1.9 and 14 nM for LDHA and LDHB, respectively).</p>

<p>SHIP2-IN-1 is a potent SHIP2 inhibitor(IC50 : 2 µM),and used in the research of Alzheimer’s disease.</p>

<p>T-0156 is a PEG5 inhibitor that inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) with low affinity for PDE6, PDE1, PDE2, PDE3 and PDE4.</p>

<p>This assay employs the competitive inhibition enzyme immunoassay technique. The microtiter plate provided in this kit has been pre-coated with Rat PⅠNP protein. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Rat PⅠNP. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Rat PⅠNP in the samples is then determined by comparing the OD of the samples to the standard curve.</p>

<p>Gamibetal (4-Amino-3-hydroxybutyric Acid) is used as a chiral reagent in the synthesis of antiepileptic and hypotensive drug GABOB and analogues.</p>

<p>N4-Acetylcytidine triphosphate is efficiently used as a substrate in T7 Polymerase-catalyzed in vitro transcription .</p>

<p>T3 Acyl glucuronide is the acyl glucuronide formation of triiodothyronine (T3). T3 Acyl glucuronide is an endogenous metabolite</p>

<p>CD13-IN-1 (Compound 5f) is a CD13 inhibitor with an IC50 value of 1.71 μM. It effectively suppresses the proliferation of various tumor cells, demonstrating antitumor activity.</p>

<p>Methylcardol triene, a phenolic compound present in cashew nut shell liquid, demonstrates α-glucosidase inhibition (IC50= 39.6 µM) and exhibits schistosomicidal properties by eliminating 100% of adult S. mansoni worms within 24 hours at 100 and 200 µM concentrations. Moreover, it serves as a precursor for synthesizing mono- and bis-benzoxazines.</p>

<p>N-Desethyl Bimatoprost (17-phenyl trinor PGF2α amide) is an F-series PG analog in which the C-1 carboxyl group has been modified to an unsubstituted amide.</p>

<p>5′-Nucleotidase (CD73), an ectoenzyme and intrinsic membrane glycoprotein, catalyzes the hydrolysis of 5-nucleotides into their corresponding nucleosides [1].</p>

<p>Calcitetrol is the hormonally active form of vitamin D with three hydroxyl groups.</p>

<p>THX6 is an activator of human mitochondrial protease ClpP, with an EC50 of 1.18 μM. It displays cytotoxicity in ONC201-resistant SU-DIPG-VI cells, with an IC50 of 0.13 μM. THX6 inhibits the expression of mitochondria-related proteins (such as parkin, TFAM, NRF1, SDHA), leading to impaired mitochondrial function. Additionally, THX6 affects cell membrane lipid metabolism and exhibits antitumor potential.</p>

<p>Cis-Vitamin K1 is an endogenous metabolite of Vitamin K [1] .</p>

<p>Picornain 3C, a protease in picornaviruses, cleaves Gln-Gly bonds in poliovirus polyproteins and similar sites in others.</p>

<p>NU227326 is a PROTAC degrader of indoleamine 2,3-dioxygenase 1 (IDO1) with a DC50 value of 4.5 nM. It effectively degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively. NU227326 exhibits favorable pharmacokinetic properties, with a plasma half-life of 5.7 hours and a brain tissue half-life of 11.8 hours. (Pink: ligand for target protein IDO1 ligand-1; Black: linker; Blue: ligand for E3 ligase Cereblon).</p>

<p>Cyclopenol is a natural product that can be used as a reference standard. The CAS number of Cyclopenol is 20007-85-6.</p>

<p>6-Azathymine is a metabolite of Pymetrozine, an insecticide targeting aphids and whiteflies by disrupting feeding.</p>

<p>24, 25-Dihydroxy VD3 is closely related to 1,25-dihydroxy vitamin D3, the active form of vitamin D3.</p>

<p>11,12-DiHETrE: Endogenous P450 eicosanoid, used in preterm labor study and NAFL/NASH differentiation.</p>

<p>Venetoclax N-oxide is a byproduct of potent, oral Bcl-2 inhibitor Venetoclax (ABT-199/GDC-0199) with Ki &lt;0.01 nM.</p>

<p>ARL67156 trisodium hydrate inhibits ecto-ATPase, NTPDase1, NTPDase3, NPP1 (Kis 11-18µM), for calcific valve disease, asthma research.</p>

<p>DSPE-PEG1000-M2pep is a PEG compound comprised of DSPE and the M2 macrophage-targeting peptide (M2pep). M2pep acts as a mono- or multivalent ligand conjugated with pro-apoptotic peptides to focus the peptides' toxic effects on M2 macrophages. DSPE-PEG1000-M2pep can be utilized for drug delivery.</p>

<p>Cidofovir diphosphate triethylamine: active metabolite inhibiting HCMV, HSV-1, HSV-2 DNA polymerases with K i values 6.6, 0.86, 1.4 μM.</p>

<p>Geranylgeranyl pyrophosphate: a metabolite for protein modification and diterpenoid precursor, used in cancer research.</p>

<p>Maltodextrin (DE 16.5-19.5) is an inactive pharma excipient that enhances drug stability, solubility, and processing.</p>

<p>Larsucosterol sodium: a liver-derived cholesterol byproduct; modulates lipid synthesis, inflammation, and cell death regulation.</p>

<p>Isoglycycoumarin, a flavonoid derived from the roots of Glycyrrhiza uralensis, serves as a highly selective probe for human cytochrome P450 2A6.</p>

<p>Decanoyl coenzyme A (Decanoyl CoA) serves as a primer for the fatty acid elongation system in Mycobacterium smegmatis [1].</p>

<p>D-Fructose 1-phosphate disodium salt, a derivative of fructose, serves as a crucial intermediate in glucose metabolism.</p>

<p>Prostaglandin F2β (PGF2β) is the 9β-hydroxy stereoisomer of PGF2α.</p>

<p>Hydroxypyruvic acid: a metabolic intermediate for glycine, serine, threonine; used by serine-pyruvate aminotransferase, glyoxylate reductase.</p>

<p>(±)8-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro.</p>

<p>MCU-i11 is a novel negative modulator of the MCU, binding MICU1 and impairing muscle cell growth.</p>

<p>PROTAC PTPN2 degrader-1, a strong PTPN2 eliminator, may aid cancer/metabolic disease research.</p>

<p>Doxorubicinol is the major circulating metabolite of doxorubicin with antineoplastic acitivity.</p>

<p>Malonyl CoA: needed for fat creation, stops fat breakdown, reversibly inhibits CPT1 in mitochondria.</p>

<p>N-Acetyl-α-D-glucosamine 1-phosphate disodium (GlcNAc-1-P), an anomeric sugar phosphate, plays a crucial role as an intermediate in the biosynthesis of N-linked</p>

<p>Aeruginosin B is a biochemical.</p>

<p>Cecropin B is a small antibacterial peptide from the giant silkmoth, Hyalophora cecropia.</p>

<p>Galactonic acid, derived from galactose metabolism, is converted from galactonolactone.</p>

<p>SHP2-D26: potent SHP2 degrader binding VHL-1/SHP2, neddylation &amp; proteasome-dependent.</p>

<p>DSPE-PEG2000-CSTSMLKAC is a PEG compound composed of DSPE and CSTSMLKAC. CSTSMLKAC can mediate phage selective homing to ischemic heart tissue. DSPE-PEG2000-CSTSMLKAC is suitable for drug delivery.</p>

<p>DSPE-PEG1000-PP1 is a PEG compound composed of DSPE and the PP1 peptide. The PP1 peptide targets inflammatory atherosclerotic plaques. DSPE-PEG1000-PP1 is suitable for drug delivery applications.</p>

<p>Compound 8g (hCA/VEGFR-2-IN-2) is an indolinonylbenzenesulfonamide identified as a potential dual inhibitor targeting cancer-associated isozymes hCA IX/XII and</p>

<p>hCA IX-IN-1 inhibits hCA I/II/IX/XII with Ki of 331.4/28.4/9.4/17.8 nM, has anticancer properties.</p>

<p>Theodrenaline hydrochloride is an inhibitor targeting SARS-CoV-2 for the study of hypotension induced by spinal anesthesia.</p>

<p>5-Formylcytosine (5FC) is a rare mammalian DNA base aiding in demethylation, altering helix structure, and affecting RNA polymerase II activity.</p>

<p>Desoxycarbadox, derived from Carbadox, is a quinoxaline-di-N-oxide antibiotic compound.</p>

<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.</p>

<p>Opevesostat (ODM-208) is an inhibitor of lyase (CYP11A1) (the enzyme cleavage cholesterol side chain).</p>

<p>CanineFactor Xa is derived from purified Canine Factor X through activation by Russell's Viper Venom, after which the venom is removed.</p>

<p>PROTACMAGLdegrader-1 is an orally active PROTAC agent that simultaneously targets both monoacylglycerol lipase (MAGL) and the E3 ubiquitin ligase MDM2. It functions by degrading MAGL and inhibiting the interaction between MDM2 and p53. Additionally, PROTACMAGLdegrader-1 has partial blood-brain barrier (BBB) penetration and can induce apoptosis in glioblastoma stem cells (GSC).</p>

<p>UDP-α-D-Glucose sodium hydrate is an endogenous metabolite and a pyrimidine nucleotide sugar, involved in glycosylation reactions during metabolic</p>

<p>Carbonic anhydrase inhibitor30 (compound 17) is an inhibitor of carbonic anhydrase with Ki values of 2.13 μM for hCA I and 0.161 μM for hCA II[1].</p>

<p>BIRM 271 is a novel arachidonic acid release inhibitor that blocks leukotriene B4 and platelet-activating factor biosynthesis in human neutrophils.</p>

<p>N-Formyl-2-aminophenol (N-(2-hydroxyphenyl)methanamide) is a bacterial secondary metabolite found in P. chrysogenum and exhibits antioxidant properties.</p>

<p>DHODH-IN-23 is a DHODH inhibitor with oral activity. DHODH-IN-23 is often used in cancer research.</p>

<p>Laprafylline: Xanthine derivative, blocks bronchoconstriction &amp; tumor growth, competes with serotonin, resists histamine at high levels.</p>

<p>RORγ inverse agonist 1 has anti-inflammatory activity and can be used to treat rheumatism and psoriasis.</p>

<p>6-hydroxy Chlorzoxazone, a chlorzoxazone metabolite, is formed in the liver via CYP2E1.</p>

<p>N-acetyl Dapsone is an anti-inflammatory and antimicrobial compound widely used in the treatment of leprosy, malaria, acne and various immune disorders.</p>

<p>3,3'-Bipyridine is an inhibitor of CYP2A6, CYP3A4, and CYP2B6, and also inhibits gastric acid secretion in rats.</p>

<p>AM6701 is a novel highly potent inhibitor of human alpha/beta hydrolase domain 6 (habhd6)</p>

<p>Oseltamivir carboxylate is an active metabolite of oseltamivir phosphate (Tamiflu).</p>

<p>Desbutyl Lumefantrine is a metabolite of lumefantrine with antimalarial activity.</p>

<p>Atorvastatin Epoxy Tetrahydrofuran: an impurity from Atorvastatin oxidation; it's an oral HMG-CoA reductase inhibitor.</p>

<p>Tetrahydrothiophen-3-one can be used as food spices.</p>

<p>Dihydrozeatin riboside is a cytokinin that can be isolated from Phaseolus vulgaris L.</p>

<p>FPI-1523 sodium, avibactam derivative; β-lactamase inhibitor (Kd: CTX-M-15, 4nM; OXA-48, 34nM); PBP2 inhibitor (IC50, 3.2μM); strong antibacterial.</p>

<p>PDE2A-IN-1 is a phosphodiesterase 2A (PDE2A) inhibitor with an IC 50 value of 1.3 nM.</p>

<p>MS1262-C3-amide-C10-amine is an E3 Ligase Ligand-Linker conjugate. It includes a GLP ligand targeting the E3 ligase SPOP and a PROTAC linker. This compound can be utilized in designing PROTACs such as example [MS479].</p>

<p>(±)13(14)-DiHDPA is a metabolite of docosahexaenoic acid that is produced via oxidation by cytochrome P450 epoxygenases.</p>

<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>