Naloxegol-d5 (oxalate)
目录号 : GC46183
A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Naloxegol-d5 is intended for use as an internal standard for the quantification of naloxegol by GC- or LC-MS. Naloxegol is a peripherally acting antagonist of the μ-opioid receptor (Ki = 7.42 nM; pA2 = 7.95).1 It is selective for the μ-opioid receptor over the δ-opioid receptor (Ki = 866 nM). Naloxegol also acts as a partial agonist of κ-opioid receptors in vitro (EC50 = 47 nM for [35S]GTPγS binding) but lacks activity ex vivo at concentrations up to 10 μM. In vivo, naloxegol reverses morphine-induced decreases in gastrointestinal motility and analgesia in a hot-plate assay in rats (ED50s = 23.1 and 55.4 mg/kg, respectively), demonstrating a two-fold separation for peripheral versus CNS effects. Naloxegol also exhibits a brain uptake rate comparable to atenolol, a low-permeation standard with no brain uptake, in a rat brain perfusion model.
|1. Floettmann, E., Bui, K., Sostek, M., et al. Pharmacologic profile of naloxegol, a peripherally acting μ-opioid receptor antagonist, for the treatment of opioid-induced constipation. J. Pharmacol. Exp. Ther. 361(2), 280-291 (2017).
| Cas No. | N/A | SDF | |
| Canonical SMILES | O[C@]12[C@]3(CCN(C([2H])([2H])/C([2H])=C([2H])\[2H])[C@@H]2C4)[C@](OC5=C3C4=CC=C5O)([H])[C@@H](OCCOCCOCCOCCOCCOCCOCCOC)CC1.OC(C(O)=O)=O | ||
| 分子式 | C34H48D5NO11 • C2H2O4 | 分子量 | 746.9 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3389 mL | 6.6943 mL | 13.3887 mL |
| 5 mM | 0.2678 mL | 1.3389 mL | 2.6777 mL |
| 10 mM | 0.1339 mL | 0.6694 mL | 1.3389 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
The hyperoxaluric syndromes
Endocrinol Metab Clin North Am 1990 Dec;19(4):851-67.PMID:2081515doi
oxalate is a major component of renal stones and an important determinant of calcium oxalate solubility in urine. Although the well-defined hyperoxaluric states are relatively uncommon, a significant number of patients with calcium oxalate stones have some degree of hyperoxaluria. For these reasons an understanding of both the causes of hyperoxaluria and methods of controlling oxalate synthesis and excretion is important. This review focuses on methods for the measurement of oxalate, the metabolic pathways of oxalate synthesis, the transport and excretion of oxalate, and the hyperoxaluric syndromes.
oxalate and urinary stones
World J Surg 2000 Oct;24(10):1154-9.PMID:11071450DOI:10.1007/s002680010193.
Calcium oxalate is a major component of renal stones, and its urinary concentration plays an important role in stone formation. Even a small increase in urinary oxalate has a significant impact on calcium oxalate saturation. Although primary hyperoxaluria is relatively uncommon, patients with calcium oxalate stones have some degree of hyperoxaluria. To understand the underlying causes of such hyperoxaluria, the processes of oxalate synthesis and excretion must be clarified. This article focuses on the determination of oxalate, calculation of its saturation, and the hyperoxaluric syndromes with special reference to metabolic precursors of oxalate, including ascorbic acid, glyoxylate, and glycolate.
Oxalotrophic bacteria
Res Microbiol 2003 Jul-Aug;154(6):399-407.PMID:12892846DOI:10.1016/S0923-2508(03)00112-8.
Oxalic acid and its salts are widespread in nature, as they are produced by many species of plants, algae and fungi. The bacteria, which are capable of using oxalate as a sole carbon and energy source, are described as being "oxalotrophic". Oxalotrophic bacteria do not constitute a homogeneous taxonomic group, but they do constitute a well-defined physiological group. A limited number of aerobic bacteria which are able to utilize oxalate as sole carbon and energy source have been completely described. Most of them are facultative methylotrophs and/or facultative hydrogen-oxidizing chemolithoautotrophs. In this review, the current status of the taxonomy and biodiversity of oxalotrophic bacteria in various environments, and aspects of their biotechnological potential, are briefly summarized.
Probiotics and other key determinants of dietary oxalate absorption
Adv Nutr 2011 May;2(3):254-60.PMID:22332057DOI:10.3945/an.111.000414.
oxalate is a common component of many foods of plant origin, including nuts, fruits, vegetables, grains, and legumes, and is typically present as a salt of oxalic acid. Because virtually all absorbed oxalic acid is excreted in the urine and hyperoxaluria is known to be a considerable risk factor for urolithiasis, it is important to understand the factors that have the potential to alter the efficiency of oxalate absorption. oxalate bioavailability, a term that has been used to refer to that portion of food-derived oxalate that is absorbed from the gastrointestinal tract (GIT), is estimated to range from 2 to 15% for different foods. oxalate bioavailability appears to be decreased by concomitant food ingestion due to interactions between oxalate and coingested food components that likely result in less oxalic acid remaining in a soluble form. There is a lack of consensus in the literature as to whether efficiency of oxalate absorption is dependent on the proportion of total dietary oxalate that is in a soluble form. However, studies that directly compared foods of varying soluble oxalate contents have generally supported the proposition that the amount of soluble oxalate in food is an important determinant of oxalate bioavailability. oxalate degradation by oxalate-degrading bacteria within the GIT is another key factor that could affect oxalate absorption and degree of oxaluria. Studies that have assessed the efficacy of oral ingestion of probiotics that provide bacteria with oxalate-degrading capacity have led to promising but generally mixed results, and this remains a fertile area for future studies.
Dietary oxalate and its intestinal absorption
Scanning Microsc 1995;9(4):1109-18; discussion 1118-20.PMID:8819892doi
Dietary oxalate is currently believed to make only a minor contribution (< 20%) to urinary oxalate excretion. A recent prospective study of stone disease suggested that dietary oxalate may be a significant risk factor. This observation led us to re-evaluate the contribution of dietary oxalate to urinary oxalate excretion. Previous studies have been hampered by inaccurate food composition tables for oxalate and inadequate methods for studying intestinal oxalate absorption. This evidence as well as factors that modify oxalate absorption are reviewed. New approaches to measure food oxalate and intestinal oxalate absorption have been examined. Capillary electrophoresis appears to be well suited for the analysis of the oxalate content of food. Two individuals consumed an oxalate-free formula diet for 7 days. This diet decreased urinary oxalate excretion by an average of 67% (18.6 mg per 24 hours) compared to oxalate excretion on self-selected diets. The absence of detectable oxalate in feces by day 6 of the diet suggested that the intestinal absorption was minimal. However, an effect of the formula diet on endogenous oxalate synthesis cannot be excluded. Restoring oxalate to the formula diet increased urinary oxalate excretion and illustrates that this experimental protocol may be well-suited for studying oxalate absorption and factors that modify it. Our results suggest that the intestinal absorption of dietary oxalate makes a substantial contribution to urinary oxalate excretion and that this absorption can be modified by decreasing oxalate intake or increasing the intakes of calcium, magnesium, and fiber.