Nitrogen-15 Labeled Compounds

L-Phenylalanine-15N ((S)-2-Amino-3-phenylpropionic acid-15N) 是 15N 标记的 L-Phenylalanine。L-Phenylalanine 是从大肠杆菌中分离出来的一种必需氨基酸。 L-Phenylalanine 广泛用于食品香精和药物的生产。

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.

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

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。

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

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.

Upadacitinib-15N-d2 是 Upadacitinib 的 15N 和氘代化合物。Upadacitinib 的 CAS 号为 1310726-60-3。Upadacitinib 是高效选择性的，具有口服活性的JAK1抑制剂，IC50为43 nM，可用于多种自身免疫性疾病的研究。它对 JAK1 的选择性约为 JAK2 的 74 倍。

L-Valine-13C5-15N 是 L-Valine 的 13C 和 15 N 的标记化合物。L-Valine 的 CAS 号为 72-18-4。L-Valine 是蛋白二十种氨基酸中的其中一种。它是必需氨基酸。

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.

Benzamide-15N (NSC-3114-15N) is a 15N-labeled Benzamide. Benzamide inhibits poly(ADP-ribose) polymerase (PARP).

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)

L-Glutamic acid-15N is the 15N-labeled version of L-Glutamic acid, an excitatory neurotransmitter and an agonist at metabotropic, kainate, NMDA, and AMPA glutamate receptor subtypes. It directly activates the release of dopamine (DA) from dopaminergic terminals.

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).

Gemcitabine EP Impurity C-13C-15N2 是 Gemcitabine EP Impurity C 的 13C 和 15 N 的标记化合物。

Lamivudine 13C,15N2, an impurity of Lamivudine (BCH-189), functions as an inhibitor of both HIV-1/2 reverse transcriptase and hepatitis B virus reverse transcriptase, classifying it as a nucleoside reverse transcriptase inhibitor (NRTIs).

Roxadustat-13C2-15N 是 Roxadustat 的 13C 和 15N 的标记化合物。

Glutathione-(glyucine-13C2-15N) Trifluoroacetate 是 Glutathione Trifluoroacetate 的 13C 和 15 N 的标记化合物。

L-Thyroxine-13C9,15N is intended for use as an internal standard for the quantification of L-thyroxine by GC- or LC-MS. L-Thyroxine is a synthetic form of the thyroid hormone thyroxine. In vivo, L-thyroxine (0.9 and 2.7 μg) inhibits synthesis and release of thyrotropin induced by thyrotropin-releasing hormone from the anterior pituitary in mice. It also reverses decreases in levels of circulating thymic serum factor (FTS) and the number of T rosette-forming cells in an old age-induced mouse model of hypothyroidism. Formulations containing L-thyroxine have been used in the treatment of hypothyroidism.

Cefdinir-13C-15N2 是 Cefdinir 的 13C 和 15 N 的标记化合物。Cefdinir 的 CAS 号为 91832-40-5。Cefdinir是头孢菌素类中的一种半合成广谱抗生素，对几种革兰氏阴性和革兰氏阳性细菌引起的感染有效。它可研究耳，鼻窦，喉咙和皮肤的常见细菌感染。

Semicarbazide-13C-15N2 Hydrochloride 是 Semicarbazide Hydrochloride 的 13C 和 15 N 的标记化合物。Semicarbazide Hydrochloride 的 CAS 号为 563-41-7。Semicarbazide hydrochloride 是一种尿素衍生物，能够与细胞中的铜或铁结合，产生抗病毒、抗感染和抗肿瘤作用。

Tranexamic Acid-13C2-15N 是 Tranexamic Acid 的 13C 和 15 N 的标记化合物。Tranexamic Acid 的 CAS 号为 1197-18-8。Amstat 是一种能阻断纤溶酶的赖氨酸结合位点和弹性蛋白酶来源的纤维蛋白溶酶原片段。

L-Lysine-13C6-15N2 Hydrochloride 是 L-Lysine Hydrochloride 的 13C 和 15 N 的标记化合物。L-Lysine Hydrochloride 的 CAS 号为 657-27-2。L-lysine hydrochloride 是一种人类必需氨基酸，能增加钙吸收，减少糖尿病相关疾病和改善肠道健康，可用于疱疹的研究。

L-Arginine-15N4 ((S)-(+)-Arginine-15N4) hydrochloride, the 15N-labeled variant of L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride), serves as the nitrogen donor in the synthesis of nitric oxide. This potent vasodilator is crucial, especially during a sickle cell crisis where its levels are notably diminished.

Glyphosate-13C2-15N 是 Glyphosate 的 13C 和 15 N 的标记化合物。Glyphosate 的 CAS 号为 1071-83-6。Glyphosate 是氨基酸甘氨酸的衍生物。它是一种除草剂，靶向并阻断植物合成芳香氨基酸所必需的莽草酸途径。

Zanamivir-13C,15N2is intended for use as an internal standard for the quantification of zanamivir by GC- or LC-MS. Zanamivir is a sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles.1It has been shown to selectively inhibit the growth of influenza A and B viruses in plaque reduction assays with IC50values ranging from 5 to 14 nM and to directly inhibit influenza A and B virus neuraminidases with IC50values ranging from 0.6 to 7.9 nMin vitro. Intranasal zanamivir administration at 0.4 mg kg twice daily reduces mortality and viral titers in lung homogenates of mice infected with influenza. 1.Elliott, M.Zanamivir: From drug design to the clinicPhilos. Trans. R. Soc. Lond. B Biol Sci.356(1416)1885-1893(2001)

Uric acid-13C-15N2 是 Uric acid 的 13C 和 15 N 的标记化合物。Uric acid 的 CAS 号为 69-93-2。Uric acid 是一种重要的抗氧化剂。Uric acid 能清除活性氧(ROS) ，如单线态氧和过氧亚硝酸盐，抑制脂质过氧化。Uric acid 有助于维持血压的稳定和抗氧化应激。

Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine 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). 1.Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS bindingBiochem. Pharmacol.55(7)1035-1043(1998) 2.Nikolic, K., Filipic, S., and Agbaba, D.QSAR study of imidazoline antihypertensive drugsBioorg. Med. Chem.16(15)7134-7140(2008) 3.Scholtysik, G.Pharmacology of guanfacineBr. J. Clin. Pharmacol.10(Suppl 1)21S-24S(1980) 4.Kauser, H., Sahu, S., Kumar, S., et al.Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive declineNeuroscience254110-119(2013)

3,5-Dinitrosalicylhydrazide-15N2 是 3,5-Dinitrosalicylhydrazide 的 13C 和氘代化合物。