Carbon-13 Labeled Compounds

D-Glucose-13C6 (Dextrose-13C6) 是一种 D-Glucose 的同位素标记物，可作为代谢示踪剂，可用于研究机体代谢相关疾病和部分物质的代谢过程。

Phenol-13C6 是一种 13C 标记的 Phenol。Phenol 是一种重要的化化工原材料，可用用于制造杀菌剂和除草剂。

L-Leucine-1-13C (L-Leucine-13C)是一种 13C 标记的 L-Leucine，显著增强了 GLP-4 的亲和力。

5-Fluorouracil-13C,15N2 is intended for use as an internal standard for the quantification of 5-flurouracil by GC- or LC-MS. 5-Fluorouracil is a pyrimidine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis. Intracellular metabolites of 5-fluorouracil exert cytotoxic effects by either inhibiting thymidylate synthetase, or through incorporation into RNA and DNA, ultimately initiating apoptosis.

Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1]. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer[1].Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process[2]. [1]. Moyer JD, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997, 57(21), 4838-4848.[2]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

13C-d3-AOH1996 是 AOH1996 的 13C 和氘代化合物。AOH1996 的 CAS 号为 2089314-64-5。AOH1996 是一种具有口服活性的复制体组分 PCNA (增殖细胞核抗原) 配体，靶向转录-复制冲突 (TRC)。AOH1996 可干扰 PCNA 与其结合蛋白的相互作用，导致 DNA 复制应激，诱导细胞凋亡 (apoptosis)。AOH1996 通过稳定 PCNA 和 RNA 聚合酶 II 的相互作用从而导致蛋白酶体依赖的 rpb1 降解和致命的 DNA 损伤。AOH1996 与 DNA 损伤剂具有协同作用，可抑制肿瘤细胞生长。

Sofosbuvir-13C-d3 是 Sofosbuvir 的 13C 和氘代化合物。Sofosbuvir 的 CAS 号为 1190307-88-0。Sofosbuvir 是一种丙型肝炎病毒聚合酶 NS5B 的尿苷单磷酸类似物抑制剂，用作治疗慢性丙型肝炎的抗病毒剂。

Taltirelin-13C-d3 是 Taltirelin 的 13C 和氘代化合物。Taltirelin 的 CAS 号为 103300-74-9。Taltirelin 是促甲状腺激素释放激素受体(TRH-R)超激动剂(IC50:910 nM)，能够刺激细胞溶质Ca2+浓度增加 (Ca2+释放) (EC50:36 nM)。

Riociguat-13C-d6 是 Riociguat 的 13C 和氘代化合物。Riociguat 的 CAS 号为 625115-55-1。Riociguat 是一种鸟苷酸环化酶的刺激剂，可导致血管平滑肌松弛，用于治疗严重的肺动脉高压。

Roxadustat-13C-15N 是 Roxadustat 的 13C 和 15N 的标记化合物。

3,3',5-Triiodothyronine-(tyrosine ring-13C6) 是 3,3',5-Triiodothyronine 的 13C 的标记化合物。3,3',5-Triiodothyronine 的 CAS 号为 5817-39-0。

Aflatoxin G2-13C17is 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 1.Bennett, J.W., and Klich, M.MycotoxinsClin. Microbiol. Rev.16(3)497-516(2003) 2.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins and analogsCancer Res.31(12)1936-1942(1971)

Vadadustat-13C2-15N 是 Vadadustat 的 13C 和 15N 的标记化合物。Vadadustat 的 CAS 号为 1000025-07-9。Vadadustat 是一种可滴定口服的缺氧诱导因子脯氨酰羟化酶 (HIF-PH) 抑制剂，是一种促红细胞生成剂，在动物慢性肾脏疾病模型中，有用于贫血的研究潜力。

Cyanuric acid-13C3 是 13C 标记的 Cyanuric acid。

Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid 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 is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 |1. Santos, M.J., López-Jurado, M., Llopis, J., et al. Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patients. Ann. Nutr. Metab. 39(1), 52-62 (1995).|2. Lee, J.Y., Sohn, K.H., Rhee, S.H., et al. Saturated fatty acids, but not unsaturated fatty acids, induced the expression of cyclooxygenase-2 mediated through toll-like receptor 4. J. Biol. Chem. 276(20), 16683-16689 (2001).|3. Dietzen, D.J., Hastings, W.R., and Lublin, D.M. Caveolin is palmitoylated on multiple cysteine residues. Palmitoylation is not necessary for localization of caveolin to caveolae. J. Biol. Chem. 270(12), 6838-6842 (1995).|4. Robinson, L.J., and Michel, T. Mutagenesis of palmitoylation sites in endothelial nitric oxide synthase identifies a novel motif for dual acylation and subcellular targeting. Proc. Nat. Acad. Sci. USA 92(25), 11776-11780 (1995).|5. Topinka, J.R., and Bredt, D.S. N-terminal palmitoylation of PSD-95 regulates association with cell membranes and interaction with K+ channel Kv1.4. Neuron 20(1), 125-134 (1998).|6. Miggin, S.M., Lawler, O.A., and Kinsella, B.T. Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J. Biol. Chem. 278(9), 6947-6958 (2003).

1,2-Dioleoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2-dioleoyl-rac-glycerol by GC- or LC-MS. 1,2-dioleoyl-rac-glycerol is a diacylglycerol that contains oleic acid at the sn-1 and sn-2 positions. It effectively binds the C1 domain to activate conventional protein kinase C forms and serves as a substrate for diacylglycerol kinases and multisubstrate lipid kinase.1,2,3 |1. Yamaguchi, Y., Shirai, Y., Matsubara, T., et al. Phosphorylation and up-regulation of diacylglycerol kinase γ via its interaction with protein kinase Cγ. J. Biol. Chem. 281(42), 31627-31637 (2006).|2. Zhou, Q.Z., Raynor, R.L., Wood, M.G., Jr., et al. Structure-activity relationship of synthetic branched-chain distearoylglycerol (distearin) as protein kinase C activators. Biochemistry 27(19), 7361-7365 (1988).|3. Epand, R.M., Shulga, Y.V., Timmons, H.C., et al. Substrate chirality and specificity of diacylglycerol kinases and the multisubstrate lipid kinase. Biochemistry 46(49), 14225-14231 (2007).

Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg kg. Nitisinone (3 mg kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (FAH) deficiency in mice when administered to pregnant dams.2It exhibits hepatoprotective effects inFAH- -mice, such as prevention of increases in plasma levels of aspartate serine aminotransferase (AST) and conjugated bilirubin, when administration is continued following birth at a dose of 1 mg kg. Nitisinone (100 μg) decreases urinary excretion of homogentisate and increases urinary excretion of HPPA, HPLA, and 4-hydroxyphenylacetate in a mouse model of alkaptonuria induced by ethylnitrosourea.3Formulations containing nitisinone have been used in the treatment of hereditary tyrosinemia type 1 (HT-1). 1.Ellis, M.K., Whitfield, A.C., Gowans, L.A., et al.Inhibition of 4-hydroxyphenylpyruvate dioxygenase by 2-(2-nitro-4-trifluoromethylbenzoyl)-cyclohexane-1,3-dione and 2-(2-chloro-4-methanesulfonylbenzoyl)-cyclohexane-1,3-dioneToxicol. Appl. Pharmacol.133(1)12-19(1995) 2.Grompe, M., Lindstedt, S., al-Dhalimy, M., et al.Pharmacological correction of neonatal lethal hepatic dysfunction in a murine model of hereditary tyrosinaemia type INat. Genet.10(4)453-460(1995) 3.Suzuki, Y., Oda, K., Yoshikawa, Y., et al.A novel therapeutic trial of homogentisic aciduria in a murine model of alkaptonuriaJ. Hum. Genet.44(2)79-84(1999)

L-Lactic acid-13C3 is a stable isotope labeled L-Lactic acid analog. L-Lactic acid-13C3 can be used for lactate metabolism research.

Oleic acid-13C is intended for use as an internal standard for the quantification of oleic acid by GC- or LC-MS. Oleic acid 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

1,2,3-Trioctanoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2,3-trioctanoyl-rac-glycerol by GC- or LC-MS. 1,2,3-Trioctanoyl-rac-glycerol is a triacylglycerol that contains octanoic acid at the sn-1, sn-2, and sn-3 positions. Dietary administration of 1,2,3-trioctanoyl-rac-glycerol increases hippocampal levels of the glycolytic metabolites glucose 6-phosphate, fructose 6-phosphate, and β-hydroxybutyrate and the seizure threshold in the 6 Hz psychomotor seizure test in mice.1 Formulations containing 1,2,3-trioctanoyl-rac-glycerol have been used in cosmetic products as thickening and skin-conditioning agents.

2-Nitrobenzaldehyde semicarbazone (13C, 15N2) is utilized in the LC-MS MS method for semicarbazide analysis.

4-Trifluoromethylsalicylic acid-13C6 是 13C 标记的 4-Trifluoromethylsalicylic acid，主要用于药物开发过程中的定量示踪剂。4-Trifluoromethylsalicylic acid 也是一种血小板聚集抑制剂。

Cefazolin-13C2,15N is intended for use as an internal standard for the quantification of cefazolin by GC- or LC-MS. Cefazolin is a broad-spectrum cephalosporin antibiotic that is active in vitro against various Gram-positive and Gram-negative bacteria (MICs = 0.2-12.5 μg ml). It also inhibits the growth of clinical isolates of S. aureus, E. coli, P. mirabilis, and K. pneumoniae (MICs = 0.1-25 μg ml). In vivo, cefazolin protects against S. aureus, E. coli, and P. mirabilis infection in mice (ED50s = <0.09-1.78, 0.44-3.63, and 2.31-5.2 mg animal, respectively). Formulations containing cefazolin have been used to treat a variety of bacterial infections.

Ethyl Acetate-13C2 是 Ethyl Acetate 的 13C 的标记化合物。Ethyl Acetate 的 CAS 号为 141-78-6。

Formoterol-13C-d3 Hemifumarate 是 Formoterol Hemifumarate 的 13C 和氘代化合物。Formoterol Hemifumarate 的 CAS 号为 43229-80-7。Formoterol Hemifumarate 是一种长效的 β2-肾上腺素受体激动剂。

Vancomycin-13C-d3 是 Vancomycin 的 13C 和氘代化合物。Vancomycin 的 CAS 号为 1404-90-6。Vancomycin 是一种抗生素，用于通过阻止细菌生长来治疗严重的细菌感染。它还改变细胞膜的渗透性并选择性地抑制核糖核酸的合成。

Sodium Acetate-1-13C 是 Sodium Acetate 的 13C 的标记化合物。Sodium Acetate 的 CAS 号为 127-09-3。Sodium acetate 是常用的实验室试剂。

2,4-Dichlorophenol-13C6 是 2,4-Dichlorophenol 的 13C 和氘代化合物。2,4-Dichlorophenol 的 CAS 号为 120-83-2。2,4-Dichlorophenol 是除草剂 2,4-二氯苯氧乙酸 (2,4-D) 的前体。

trans-Hydroxy Loxoprofen-13C-d3 (Mixture of Diastereomers) 是 trans-Hydroxy Loxoprofen 的 13C 和氘代化合物。trans-Hydroxy Loxoprofen 的 CAS 号为 371753-19-4。

Lercanidipine-13C-d3 HCl 是 Lercanidipine HCl 的 13C 和氘代化合物。Lercanidipine HCl 的 CAS 号为 132866-11-6。Lercanidipine hydrochloride 是亲脂性二氢吡啶-钙通道阻滞剂，具有持久的降压作用和保护肾脏作用。

Ondansetron-13C-d3 是 Ondansetron 的 13C 和氘代化合物。Ondansetron 的 CAS 号为 99614-02-5。Ondansetron 是一种血清素 5-HT3 受体拮抗剂，主要用作止吐剂。

Nicergoline-13C-d3 是 Nicergoline 的 13C 和氘代化合物。Nicergoline 的 CAS 号为 27848-84-6。Nicergoline 是一种有效的，选择性的、具有口服活性的α1A-肾上腺素能受体拮抗剂，是一种溴烟碱酸的麦角林衍生物。它具有血管舒张作用，可以改善阿尔茨海默症小鼠的认知功能。

Benzophenone-13C (carbonyl-13C) 是 Benzophenone 的 13C 的标记化合物。Benzophenone 的 CAS 号为 119-61-9。

Alosetron-13C-d3 是 Alosetron 的 13C 和氘代化合物。Alosetron 的 CAS 号为 122852-42-0。

5-Hydroxy Saxagliptin-13C-d2 HCl 是 5-Hydroxy Saxagliptin HCl 的 13C 和氘代化合物。5-Hydroxy Saxagliptin HCl 的 CAS 号为 841302-24-7。

Avanafil-13C-d3 是 Avanafil 的 13C 和氘代化合物。Avanafil 的 CAS 号为 330784-47-9。Avanafil 是一种高活性PDE-5抑制剂，IC50=5.2 nM，对PDE1，PDE6和PDE11活性较低。

Berberine hydrochloride-13C-d3 是 Berberine hydrochloride 的 13C 和氘代化合物。

Binimetinib-13C-d3 是 Binimetinib 的 13C 和氘代化合物。Binimetinib 的 CAS 号为 606143-89-9。Binimetinib 是一种可口服的选择性MEK1/2抑制剂，抑制MEK的IC50为 12 nM。

Tacrolimus-13C-d2 是 Tacrolimus 的 13C 和氘代化合物。

Prucalopride-13C-d3 是 Prucalopride 的 13C 和氘代化合物。Prucalopride 的 CAS 号为 179474-81-8。Prucalopride 是一种选择性、高亲和力的 5-HT4A/4B 受体激动剂，Ki为2.5和 8 nM。它对 5-HT4A/4B 受体的选择性是其他 5-HT 受体亚型的 290 倍以上。

L-Thyroxine-13C6 是 L-Thyroxine 的 13C 的标记化合物。L-Thyroxine 的 CAS 号为 51-48-9。L-Thyroxine (T4)是一种合成的甲状腺激素，用于甲状腺功能减退症的研究。在DIO 酶作用下， L-Thyroxine (T4)转化成具有生物特性的三碘甲状腺氨酸 (T3)。

13C C16 Sphingomyelin is an isotopically enriched form of C16 sphingomyelin with carbon-13 occurring on the fatty acid portion. It is intended for use as an internal standard for the quantification of C16 sphingomyelin by GC- or LC-MS. C16 Sphingomyelin is a form of sphingomyelin containing palmitate (16:0) at the variable acylation position. It is the most common form of sphingomyelin found in eggs and is less abundant in the brain and in milk. C16 Sphingomyelin interacts with cholesterol in ordered lipid domains (lipid rafts). Sphingomyelinases remove phosphorylcholine from C16 sphingomyelin to produce C16 ceramide. While ceramides commonly induce apoptosis, ceramides with different fatty acid chain lengths might direct distinct functions and, in some cases, reduce apoptosis.

4-deoxy Nivalenol-13C15is intended for use as an internal standard for the quantification of 4-deoxy nivalenol by GC- or LC-MS. 4-deoxy Nivalenol 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 (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. 1.Pestka, J.J., and Smolinski, A.T.Deoxynivalenol: Toxicology and potential effects on humansJ.Toxicol.Environ.Health B.Crit.Rev.8(1)39-69(2005) 2.Forsyth, D.M., Yoshizawa, T., Morooka, N., et al.Emetic and refusal activity of deoxynivalenol to swineAppl. Environ. Microbiol.34(5)547-552(1977) 3.Pestka, J.J.Deoxynivalenol: Mechanisms of action, human exposure, and toxicological relevanceArch. Toxicol.84(9)663-679(2010)

Riluzole-13C,15N2 is intended for use as an internal standard for the quantification of riluzole by GC- or LC-MS. Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED50 value of 3.2 mg kg and displays neuroprotective effects in hypoxic animals at an ED50 value of 4 mg kg. Formulations containing riluzole have been explored as therapeutics for slowing disease progression of amyotrophic lateral sclerosis.

Caffeic acid-13C3 is an isotopically enriched form of caffeic acid that is intended for use as an internal standard for the quantification of caffeic acid by GC- or LC-MS. Caffeic acid is an inhibitor of 5-LO , with IC50 values of 3.7-72 μM, and 12-LO, with IC50 values of 5.1-30 μM.

Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.3,4,5,6,7 |1. Dippold, M.A., and Kuzyakov, Y. Direct incorporation of fatty acids into microbial phospholipids in soils: Position-specific labeling tells the story. Geochim. Cosmochim. Acta 174(1), 211-221 (2016).|2. Santos, M.J., López-Jurado, M., Llopis, J., et al. Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patients. Ann. Nutr. Metab. 39(1), 52-62 (1995).|3. Lee, J.Y., Sohn, K.H., Rhee, S.H., et al. Saturated fatty acids, but not unsaturated fatty acids, induced the expression of cyclooxygenase-2 mediated through toll-like receptor 4. J. Biol. Chem. 276(20), 16683-16689 (2001).|4. Dietzen, D.J., Hastings, W.R., and Lublin, D.M. Caveolin is palmitoylated on multiple cysteine residues. Palmitoylation is not necessary for localization of caveolin to caveolae. J. Biol. Chem. 270(12), 6838-6842 (1995).|5. Robinson, L.J., and Michel, T. Mutagenesis of palmitoylation sites in endothelial nitric oxide synthase identifies a novel motif for dual acylation and subcellular targeting. Proc. Nat. Acad. Sci. USA 92(25), 11776-11780 (1995).|6. Topinka, J.R., and Bredt, D.S. N-terminal palmitoylation of PSD-95 regulates association with cell membranes and interaction with K+ channel Kv1.4. Neuron 20(1), 125-134 (1998).|7. Miggin, S.M., Lawler, O.A., and Kinsella, B.T. Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J. Biol. Chem. 278(9), 6947-6958 (2003).

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 |1. Mallatou, H., Pappa, E., and Massouras, T. Changes in free fatty acids during ripening of Teleme cheese made with ewes', goats', cows' or a mixture of ewes' and goats' milk. Int. Dairy J. 13(1-3), 211-219 (2003).|2. Hyang, C.B., Alimova, Y., Myers, T.M., et al. Short- and medium-chain fatty acids exhibit antimicrobial activity for oral microorganisms. Arch. Oral Biol. 56(7), 650-654 (2011).|3. Onkenhout, W., Venizelos, V., van der Poel, P.F.H., et al. Identification and quantification of intermediates of unsaturated fatty acid metabolism in plasma of patients with fatty acid oxidation disorders. Clin. Chem. 41(10), 1467-1474 (1995).|4. Rinaldo, P., O'Shea, J.J., Coates, P.M., et al. Medium-chain acyl-CoA dehydrogenase deficiency. Diagnosis by stable-isotope dilution measurement of urinary n-hexanoylglycine and 3-phenylpropionylglycine. N. Engl. J. Med. 319(20), 1308-1313 (1988).

L-Tyrosine-13C9,15N is intended for use as an internal standard for the quantification of L-tyrosine by GC- or LC-MS. L-Tyrosine is a non-essential amino acid.1It is produced by hydroxylation of phenylalanine by phenylalanine hydroxylase but can also be obtained from dietary sources or degradation of endogenous proteins, resulting in L-tyrosine release.1,2L-Tyrosine is a precursor in the biosynthesis of catecholamine neurotransmitters, melanins, and thyroid hormones.3Plasma, skeletal muscle, and erythrocyte levels of L-tyrosine are decreased in patients with chronic kidney disease.1 1.Kopple, J.D.Phenylalanine and tyrosine metabolism in chronic kidney failureJ. Nutr.137(6 Suppl 1)1586S-1590S(2007) 2.Webster, D., and Wildgoose, J.Tyrosine supplementation for phenylketonuriaCochrane DB Syst. Rev.2013(6)CD001507(2013) 3.Slominski, A., and Paus, R.Towards defining receptors for L-tyrosine and L-DOPAMol. Cell Endocrinol.99(2)C7-C11(1994)

rac-Hesperetin-13C-d3 是 rac-Hesperetin 的 13C 和氘代化合物。rac-Hesperetin 的 CAS 号为 69097-99-0。

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg kg, respectively). Zonisamide (40 mg kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).