Uridine-5'-diphosphoglucuronic Acid (sodium salt)
(Synonyms: 尿苷二磷酸葡萄糖醛酸三钠) 目录号 : GC45128
Uridine-5'-diphosphoglucuronic Acid（钠盐）是 P2Y14 受体的激动剂。
Cas No.:63700-19-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Microsomal incubation experimen[1]: | |
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Material |
Rat liver microsomes |
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Preparation Method |
Rat liver microsomes were incubated with 1 μM supinoxin for 60 min in the presence and absence of (A) NADPH, (B) Uridine-5'-diphosphoglucuronic Acid (UDPGA), or (C) both NADPH and UDPGA as a cofactor. |
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Applications |
Rat liver microsomes were incubated with 1 μM supinoxin. The addition of UDPGA in the NADPH-containing incubation mixture did not lead to significant metabolic profile differences from the mixture containing only NADPH, indicating the negligible contribution of UDPGA-dependent metabolism in the microsomal clearance of supinoxin. |
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References: [1]. Liu P, Wu S, et,al. Identification of the metabolites of tofacitinib in liver microsomes by liquid chromatography combined with high resolution mass spectrometry. Biomed Chromatogr. 2021 Jun;35(6):e5081. doi: 10.1002/bmc.5081. Epub 2021 Feb 10. PMID: 33522621. |
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Uridine-5'-diphosphoglucuronic Acid (sodium salt) is an agonist for the P2Y14 receptor. Uridine-5'-diphosphoglucuronic Acid (sodium salt) is also a precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and certain microorganisms, and acts as an activated form of glucose in nucleotide sugar metabolism, serving as a substrate for glucose transferase.
Rat liver microsomes were incubated with 1 μM supinoxin.The addition of Uridine-5'-diphosphoglucuronic Acid (sodium salt) in the NADPH-containing incubation mixture did not lead to significant metabolic profile differences from the mixture containing only NADPH, indicating the negligible contribution of Uridine-5'-diphosphoglucuronic Acid (sodium salt)-dependent metabolism in the microsomal clearance of supinoxin[1]. Metabolic reactions containing FDU-PB-22 and human liver microsomes (HLMs) were independent of NADPH but not Uridine-5'-diphosphoglucuronic Acid (sodium salt) [2].
References:
[1]. Liu P, Wu S, et,al. Identification of the metabolites of tofacitinib in liver microsomes by liquid chromatography combined with high resolution mass spectrometry. Biomed Chromatogr. 2021 Jun;35(6):e5081. doi: 10.1002/bmc.5081. Epub 2021 Feb 10. PMID: 33522621.
[2]. Jones S, Yarbrough AL, et,al. Enzymatic analysis of glucuronidation of synthetic cannabinoid 1-naphthyl 1-(4-fluorobenzyl)-1H-indole-3-carboxylate (FDU-PB-22). Xenobiotica. 2019 Dec;49(12):1388-1395. doi: 10.1080/00498254.2019.1580403. Epub 2019 Mar 20. PMID: 30739533; PMCID: PMC7133092.
Uridine-5'-diphosphoglucuronic Acid（钠盐）是 P2Y14 受体的激动剂。 Uridine-5'-diphosphoglucuronic Acid (sodium salt) 也是动物组织和某些微生物中含葡萄糖的低聚糖、多糖、糖蛋白和糖脂的前体，在核苷酸糖代谢中作为葡萄糖的活化形式，作为葡萄糖转移酶底物。
大鼠肝微粒体与 1 μM supinoxin 一起孵育。在含有 NADPH 的孵育混合物中添加 Uridine-5'-diphosphoglucuronic Acid（钠盐）不会导致与仅含有 NADPH 的混合物的显着代谢特征差异，表明Uridine-5'-二磷酸葡萄糖醛酸（钠盐）依赖性代谢对 supinoxin 微粒体清除的贡献可忽略不计[1]。含有 FDU-PB-22 和人肝微粒体 (HLM) 的代谢反应不依赖于 NADPH，但不依赖于尿苷 5'-二磷酸葡萄糖醛酸（钠盐）[2]。
| Cas No. | 63700-19-6 | SDF | |
| 别名 | 尿苷二磷酸葡萄糖醛酸三钠 | ||
| Canonical SMILES | O=P(OP(OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C=CC(NC2=O)=O)O1)([O-])=O)([O-])O[C@H]3O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]3O.[Na+].[Na+].[Na+] | ||
| 分子式 | C15H19N2O18P2•3Na | 分子量 | 646.2 |
| 溶解度 | H2O : 125 mg/mL (193.43 mM; Need ultrasonic); DMSO : 20 mg/mL (30.95 mM; Need ultrasonic (<50°C)) | 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 | 1.5475 mL | 7.7375 mL | 15.4751 mL |
| 5 mM | 0.3095 mL | 1.5475 mL | 3.095 mL |
| 10 mM | 0.1548 mL | 0.7738 mL | 1.5475 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。
Localization and characterization of drug-metabolizing enzymes along the villus-crypt surface of the rat small intestine--II. Conjugases
Biochem Pharmacol 1988 Jan 15;37(2):177-84.PMID:3124855DOI:10.1016/0006-2952(88)90715-0
The potential of the epithelial cells of the villus-to-crypt surface of the small intestine of the rat to conjugate xenobiotics was studied. The cells were isolated sequentially in the villus-to-crypt gradient and were found to exhibit heterogeneous distribution patterns and inducer-sensitivities of the conjugating enzymes and their cofactors. UDP-glucuronosyltransferase (GT) activities towards 3-hydroxybenzo[a]pyrene (GT1) and 4-hydroxybiphenyl (GT2) were present in all the cells. The mature upper villus cells were rich in both GT1 and GT2 activities, which declined toward the highly replicating undifferentiated crypt cells. The specific enzyme activities were four times lower in crypt cells than in upper villus cells. The presence of GT1 activity always predominated over GT2 activity. 3-Methylcholanthrene (3-MC) given orally increased GT1 activity by 2-fold in villus cells and about 6-fold in crypt cells, while phenobarbital sodium salt (PB) also markedly induced GT1 of the crypt region. Unlike GT1, GT2 activity was distinctly induced only by PB in all the cells. Both GT1 and GT2 of crypt cells were highly sensitive to inducers, in comparison to the villus cells. The uridine-5-diphosphoglucuronic acid (UDPGA) content ranged from about 0.07 to 0.2 mM in cells from crypts to villus-tip respectively. 3-MC caused a 3-fold increase in UDPGA content in all the cells; PB, however, did not affect UDPGA. The highest glutathione-S-transferase (GST) activity, however, was towards the substrate 1-chloro-2,4-dinitrobenzene; the basal specific enzyme activity varied from about 0.05 to 0.2 mumol per min per mg protein in cells from crypt to upper villus. The enzyme was induced by both types of inducers, being about 2-fold in villus cells and 3- to 5-fold in crypt cells. In contrast, the GSH content was lower in cells with higher GST activity. The endogenous GSH content ranged from 0.8 mM in the upper-villus cells to 3 mM in the crypt cells. The GSH content, however, was not altered by 3-MC or PB treatment of rats. The results demonstrate that xenobiotic conjugation reactions in intestinal cells are much stronger than monooxygenase reactions. The differential and higher sensitivity of the intestinal cells to inducers appears to provide protection to the intestine against xenobiotics during intestinal "first pass".