lc-ms

MAK683 是胚胎外胚层发育 (EED) 抑制剂。在 EED Alphascreen 结合、LC-MS 和 ELISA 测定中，IC50值为 59、89 和 26 nM。

MAK683 hydrochloride胚胎外胚层发育 (EED) 抑制剂，也是一种高效的 PRC2 抑制剂，可阻断癌细胞增殖（IC50=1.014），在EED Alphascreen， ELISA 和 LC-MS 试验中测得的IC50 值分别为 59，26，89 nM。

Dansyl glutathione是一种荧光标记的谷胱甘肽衍生物，用于检测活性代谢物。它能显著提高 LC-MS/MS 分析的灵敏度，常用于早期药物诱导毒性的体外筛选。

TAK632 是一种有效的pan-RAF 抑制剂，对CRAF、BRAFV600E 和BRAFWT 的IC50分别为 1.4、2.4 和 8.3 nM。

13C15-Nivalenol is intended for use as an internal standard for the quantification of nivalenol by GC- or LC-MS. Nivalenol (T13797) is a trichothecene mycotoxin that has been found inFusarium.1It is lethal to mice (LD50= 6.9 mg/kg).2Nivalenol (5,10,and 15 mg/kg)also induces thymic,splenic,and Peyer's patch cell apoptosis in mice.3

3-Acetyldeoxy Nivalenol-13C17 is intended for use as an internal standard for the quantification of 3-acetyldeoxy nivalenol by GC- or LC-MS. 3-Acetyldeoxy nivalenol is a mycotoxin that has been found inF. graminearum.1

4-deoxy Nivalenol-13C15 is intended for use as an internal standard for the quantification of 4-deoxy nivalenol by GC- or LC-MS. 4-deoxy Nivalenol (T15097) is a trichothecene mycotoxin that has been found inFusarium.1It binds to eukaryotic ribosomes and inhibits protein synthesis in mice when administered at doses ranging from 5 to 25 mg/kg. 4-deoxy Nivalenol (T15097) (0.1 and 0.2 mg/kg)induces emesis in pigs and decreases feed consumption in pigs when administered at a dose of 40 ppb in the diet.2It induces lethality in mice (LD50= 46-78 mg/kg).34-deoxy Nivalenol has been found inF. graminearum-infected cereal grains such as wheat,barley,and corn.

Aflatoxin B2-13C17 is intended for use as an internal standard for the quantification of AFB2by GC- or LC-MS. AFB2is a mycotoxin that has been found inA. terricola.1It induces hepatic autophagy and apoptosis in broiler chickens when administered at doses of 0.2,0.4,and 0.8 mg/kg.2AFB2 (0.5 and 1 mg/animal)also induces parenchymal cell hyperplasia in rats.3

Aflatoxin G1-13C17 is intended for use as an internal standard for the quantification of aflatoxin G1by GC- or LC-MS. Aflatoxin G1is a mycotoxin that has been found inA. terricola.1

Aflatoxin G2-13C17 is intended for use as an internal standard for the quantification of aflatoxin G2by GC- or LC-MS. Aflatoxin G2is a mycotoxin that has been found inAspergillus.1It is lethal to ducklings (LD50= 2.83 mg/kg)but is non-toxic to rats when administered at a dose of 200 mg/kg.2

Guanfacine-13C,15N3 is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine (T22824) is an α2-adrenergic receptor (α2-AR)agonist with Kivalues of 93,1,380,and 3,890 nM for α2A-,α2B-,and α2C-ARs,respectively,in a radioligand binding assay.1It has EC50values of 52,288,and 602 nM for α2A-,α2B-,and α2C-ARs,respectively,for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg/kg)binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).

O-Des[2-aminoethyl]-O-carboxymethyl dehydroamlodipine is a major metabolite of the calcium channel inhibitor amlodipine .1 1.Taguchi, R., Naito, T., Sato, H., et al.Validated LC-MS/MS method for the simultaneous determination of amlodipine and its major metabolites in human plasma of hypertensive patientsTher. Drug Monit.39(6)625-631(2017)

D-Fructose-13C6 可用作通过 GC-或 LC-MS 定量 D-果糖的内标。

2-deoxy-D-Glucose-13C is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose (T6742) is a glucose antimetabolite and an inhibitor of glycolysis. It inhibits hexokinase,the enzyme that converts glucose to glucose-6-phosphate,as well as phosphoglucose isomerase,the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.

Oleic Acid-13C is intended for use as an internal standard for the quantification of oleic acid by GC- or LC-MS. Oleic Acid (T2O2668) is a monounsaturated fatty acid and a major component of membrane phospholipids that has been found in human plasma,cell membranes,and adipose tissue.1,2 It contributes approximately 17% of the total fatty acids esterified to phosphatidylcholine,the major phospholipid class in porcine platelets.1 Oleic acid inhibits collagen-stimulated platelet aggregation by approximately 90% when used at a concentration of 10 μg/ml. It also inhibits fMLF-induced neutrophil aggregation and degranulation by 55 and 68%,respectively,when used at a concentration of 5 μM,similar to arachidonic acid .3 Oleic acid (60 μM)induces release of intracellular calcium in human platelets.4

Lauric Acid-13C is intended for use as an internal standard for the quantification of lauric acid by GC- or LC-MS. Lauric acid is a medium-chain saturated fatty acid. It has been found at high levels in coconut oil.1Lauric acid induces the activation of NF-κB and the expression of COX-2,inducible nitric oxide synthase (iNOS),and IL-1α in RAW 264.7 cells when used at a concentration of 25 μM.2

Octanoic Acid-13C is intended for use as an internal standard for the quantification of octanoic acid by GC- or LC-MS. Octanoic acid is a medium-chain saturated fatty acid. It has been found in Teleme cheeses made from goat,ovine,or bovine milk.1 Octanoic acid is active against the bacteria S. mutans,S. gordonii,F. nucleatum,and P. gingivalis (IC80s = <125,<125,1,403,and 2,294 μM,respectively).2 Levels of octanoic acid are increased in the plasma of patients with medium-chain acyl-CoA dehydrogenase (MCAD)deficiency,an inborn error of fatty acid metabolism characterized by hypoketotic hypoglycemia,medium-chain dicarboxylic aciduria,and intolerance to fasting.3,4

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)

Gliotoxin-13C13 is intended for use as an internal standard for the quantification of gliotoxin by GC- or LC-MS. Gliotoxin (TN1694) is an immunosuppressive mycotoxin produced by pathogenic strains ofAspergillusand other fungi with diverse biological activities.1,2,3,4,5,6,7,8It inhibits 20S proteasomal chymotrypsin activity (IC50= 10 μM),blocking the degradation of IκBα and preventing the activation of NF-κB.2,3Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutrophils.4,5It suppresses viral infection by Nipah and Hendra virus in HEK293T cells (IC50s = 149 and 579 nM,respectively).6Under reducing conditions,gliotoxin inhibits leukotriene A4hydrolase epoxide hydrolase activity,but not aminopeptidase activity,and leukotriene B4synthesis in neutrophils and monocytes.7

HT-2 Toxin-13C22 is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active,deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin,HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2,A549,HEp-2,Caco-2,A-204,U937,Jurkat,and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human umbilical vein endothelial cells with an IC50value of 56.4 ng/ml.1It induces oxidative stress,DNA damage,and autophagy in,as well as halts the development of,cultured mouse embryos when used at a concentration of 10 nM.3HT-2 toxin has been found in cereal grains and food products.4,5

Ochratoxin A-13C20 is intended for use as an internal standard for the quantification of ochratoxin A by GC- or LC-MS. Ochratoxin A (T75659) is a mycotoxin that has been found inAspergillusandPenicillium.1It increases lipid peroxide levels and the number of apoptotic cells,as well as reduces superoxide dismutase activity in rat kidney when administered at a dose of 120 μg/kg.2Topical application of ochratoxin A (80 μg/mouse)induces DNA damage,cell cycle arrest at the G0/G1phase,and apoptosis in mouse skin cells.1It also initiates tumor formation in a two-stage mouse skin tumorigenesis model. Ochratoxin A (T75659)has been found as a contaminant in a variety of foods.3

Zearalenone-13C18 is intended for use as an internal standard for the quantification of zearalenone by GC- or LC-MS. Zearalenone (T5625) is a mycotoxin that has been found inFusariumand has estrogenic activities.1It binds to human estrogen receptor α (ERα)and ERβ (IC50s = 9 and 5.8 nM,respectively).2Zearalenone induces precocious development of mammary tissues in young female pigs and prepucial enlargement in young male pigs.3Zearalenone (1.5-5 mg/kg of diet)induces hyperestrogenism in pigs. It also induces degeneration of meiotic chromatin in oocytes and reduces fertility in pigs when administered at a dose of 200 μg/kg.4Zearalenone has been found as a contaminant in wheat,maize,and barley and livestock feeds.3,4

Palmitic acid-1-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid (T2908) is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid (T2908) is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6

Palmitic acid-1,2,3,4-13C4 is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid (T2908) is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids,respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellular proteins,promotes protein-vesicle interactions,and regulates various G protein-coupled receptor functions.1Red blood cell palmitic acid levels are increased in patients with metabolic syndrome compared to patients without metabolic syndrome and are also increased in the plasma of patients with type 2 diabetes compared to individuals without diabetes.3,4