Tolmetin sodium dihydrate, a non-steroidal anti-inflammatory drug (NSAID), is a potent and orally active inhibitor of COX (cyclooxygenase). Its IC 50 values for human COX-1 and COX-2 are 0.35 μM and 0.82 μM, respectively [1] [2].
2'-Deoxyguanosine 5'-monophosphate (dGMP) is used as a substrate of guanylate kinases to generate dGDP, which in turn is phosphorylated to dGTP, a nucleotide precursor used in DNA synthesis. In addition, dGMP can be efficiently phosphorylated by the type I thymidylate kinase of the malarial agent P. falciparum. In humans, deficiency of mitochondrial deoxyguanosine kinase, which synthesizes dGMP from ATP and deoxyguanosine, contributes to mitochondrial DNA depletion syndrome.
N-desmethyl Rosuvastatin is an active metabolite of the HMG-CoA reductase inhibitor rosuvastatin .1,2N-desmethyl Rosuvastatin is formed when rosuvastatin undergoes demethylation, primarily by the cytochrome P450 (CYP) isoform CYP2C9 and to a lesser extent by CYP2C19 and CYP3A4.1 1.Macwan, J.S., Ionita, I.A., and Akhlaghi, F.A simple assay for the simultaneous determination of rosuvastatin acid, rosuvastatin-5S-lactone, and N-desmethyl rosuvastatin in human plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS)Anal. Bioanal. Chem.402(3)1217-1227(2012) 2.Bai, X., Wang, X.P., He, G.D., et al.Simultaneous determination of rosuvastatin, rosuvastatin-5 S-lactone, and N-desmethyl rosuvastatin in human plasma by UPLC-MS/MS and its application to clinical studyDrug Res. (Stuttg.)68(6)328-334(2018)
NADP+ is the oxidized form of the electron donor nicotinamide adenine dinucleotide phosphate . It serves as a cofactor in various biological reactions. In addition, the balance between these reduced and oxidized forms plays key roles in diverse cellular functions, including cell survival, the maintenance of redox status, and intracellular signaling. For example, binding of NADP+ to β-subunits of Kv channels activates ion transport, whereas NADPH stabilizes channel inactivation. NADP+ is biosynthesized from NAD+ by NAD kinase, with ATP as the phosphoryl donor.
Uridine-5’-monophosphate (UMP) is a ribonucleotide.1It is formedviadecarboxylation of orotidine-5’-monophosphate (5’-OMP) by OMP decarboxylase. UMP is further phosphorylated by UMP-CMP kinase to form UDP and UTP during nucleic acid biosynthesis. Formulations containing UMP have been used as dietary supplements. 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Nucleotide BiosynthesisBiochemistry(2002)
Cefsulodin is a β-lactam antibiotic that lyses actively-growingE. coliby binding specifically to the intermembrane proteins, penicillin-binding proteins 1a and b, whose transglycosylase and transpeptidase activities are involved in cell elongation and septation.1Cefsulodin has been used in combination with other β-lactam antibiotics, such as cefazolin as a strategy to circumvent drug resistance.2
Guanosine 5’-diphosphate (GDP) is a purine nucleotide and biosynthetic precursor of guanosine 5’-triphosphate .1It has been used to study the conformations of GTPases.2GDP (100 μM) activates sulfonylurea receptor 2B (SUR2B) linked to the inward-rectifier potassium channel 6.1 (Kir6.1) in HEK293T cells in a patch-clamp assay.3 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Biochemistry(2002) 2.Vetter, I.R., and Wittinghofer, A.The guanine nucleotide-binding switch in three dimensionsScience294(5545)1299-1304(2001) 3.Yamada, M., Isomoto, S., Matsumoto, S., et al.Sulphonylurea receptor 2B and Kir6.1 form a sulphonylurea-sensitive but ATP-insensitive K+ channelJ. Physiol.499(Pt 3)715-720(1997)
2'-Deoxyadenosine-5'-triphosphate (dATP) is a purine nucleotide and derivative of the nucleic acid adenosine 5'-triphosphate .1dATP is a substrate for DNA polymerase in the synthesis of DNA.2It is a noncompetitive inhibitor of ribonucleotide reductases, which provides feedback inhibition during DNA synthesis.1dATP has commonly been used in DNA synthesis, sequencing, and labeling in research applications.3,4dATP accumulates in adenosine deaminase deficiency, a disorder characterized by mutations in the gene for adenosine deaminase, the enzyme that catalyzes the deamination of adenosine and deoxyadenosine.5 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Key steps in nucleotide biosynthesis are regulated by feedback inhibitionBiochemistry(2002) 2.Berg, J.M., Tymoczko, J.L., and Stryer, L.DNA is replicated by polymerases that take instructions from templatesBiochemistry(2002) 3.Cadwell, R.C., and Joyce, G.F.Randomization of genes by PCR mutagenesisPCR Methods Appl.2(1)28-33(1992) 4.Steffens, D.L., Jang, G.Y., Sutter, S.L., et al.An infrared fluorescent dATP for labeling DNAGenome Res.5(4)393-399(1995) 5.Flinn, A.M., and Gennery, A.R.Adenosine deaminase deficiency: A reviewOrphanet J. Rare Dis.13(1)65(2018)
Riboflavin 5'-monophosphate (FMN) is a coenzyme that is tightly bound to enzymes catalyzing oxidation and reduction reactions in a variety of biosynthetic pathways. FMN also binds the FMN riboswitch (RFN element) on RNA to alter gene regulation. FMN is a substrate of FMN phosphohydrolases and is used to study their function.
UDP-α-D-Glucose is an endogenous nucleotide sugar involved in glycosyltransferase reactions in metabolism. It has been shown to bind the P2Y14receptor (EC50= 0.35 μM), an atypical P2Y receptor involved in the activation of dendritic cells and glial cells.1It can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.2 1.Jacobson, K.A., Ivanov, A.A., de Castro, S., et al.Development of selective agonists and antagonists of P2Y receptorsPurinergic Signal.5(1)75-89(2009) 2.Lecca, D., Trincavelli, M.L., Gelosa, P., et al.The recently identified P2Y-like receptor GPR17 is a sensor of brain damage and a new target for brain repairPLoS One3(10)(2008)
UDP-Glucuronic acid is a nucleoside diphosphate sugar that is a source of glucuronic acid for polysaccharide biosynthesis. This compound can be used for the formation of many glucuronides with various aglycones.1 1.Green, M.D., and Tephly, T.R.Glucuronidation of amine substrates by purified and expressed UDP-glucuronosyltransferase proteinsDrug Metab. Dispos.26(9)860-867(1998)
UDP-N-acetyl-D-Glucosamine is a natural nucleotide sugar that is used by glycosyltransferases to transfer N-acetyl-D-glucosamine residues to substrates.1It is an important component of antibiotic biosynthesis pathways in fungi and lipopolysaccharide production in bacteria.2,3 1.Roseman, S.Reflections on glycobiologyJ. Biol. Chem.276(45)41527-41542(2001) 2.Kudo, F., and Eguchi, T.Biosynthetic genes for aminoglycoside antibioticsJ. Antibiot. (Tokyo)62(9)471-481(2009) 3.Mulrooney, E.F., Poon, K.K., McNally, D.J., et al.Biosynthesis of UDP-N-acetyl-L-fucosamine, a precursor to the biosynthesis of lipopolysaccharide in Pseudomonas aeruginosa serotype O11J. Biol. Chem.280(20)19535-19542(2005)
Uridine-5'-diphosphoglucuronic acid is a nucleoside diphosphate sugar that is a source of glucuronic acid for polysaccharide biosynthesis. This compound can be used for the formation of many glucuronides with various aglycones.1 1.Green, M.D., and Tephly, T.R.Glucuronidation of amine substrates by purified and expressed UDP-glucuronosyltransferase proteinsDrug Metab. Dispos.26(9)860-867(1998)
Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)
Cromolyn is a chromone complex that acts as a mast cell stabilizer, preventing the release of histamine. Its mechanism of action is thought to involve an interference with the antigen-stimulated calcium transport across the mast cell membrane, thereby inhibiting mast cell release of histamine, leukotrienes, and other substances that cause hypersensitivity reactions.
1,3,6,8-Pyrenetetrasulfonic acid is an intermediate in the synthesis of the color additive pyranine.1It has been used to stabilize intermolecular interactions for the crystallization ofL. mexicanapyruvate kinase.2 1.Jitian, S., White, S.R., Yang, H.-H.W., et al.Conventional high-performance liquid chromatography versus derivative spectrophotometry for the determination of 1,3,6-pyrenetrisulfonic acid trisodium salt and 1,3,6,8-pyrenetetrasulfonic acid tetrasodium salt in the color additive D&C Green No. 8 (Pyranine)J. Chromatogr. A1324238-241(2014) 2.Morgan, H.P., McNae, I.W., Hsin, K.-Y., et al.An improved strategy for the crystallization of Leishmania mexicana pyruvate kinaseActa Crystallogr. Sect. F Struct. Biol. Cryst. Commun.66(Pt 3)215-218(2010)
Meclofenamate sodium is a potent non-steroidal anti-inflammatory agent, which can specifically inhibit chemokine-induced human polymorphonuclear leukocyte function: chemotaxis, degranulation, and superoxide anion free radical production.
Prasterone is an endogenous steroid hormone. Prasterone acts as an agonist at ERβ, NMDA, and σ1 receptors, a partial agonist at ERα and AR, and antagonist at GABA-A receptors. It displays a variety of biologocial activities, including enhancing working me