Uridine diphosphate glucose
(Synonyms: UDP-葡萄糖) 目录号 : GC37866
尿苷二磷酸葡萄糖（尿嘧啶二磷酸葡萄糖，UDPG）是一种核苷酸糖。
Cas No.:133-89-1
Sample solution is provided at 25 µL, 10mM.
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Uridine diphosphate glucose (uracil-diphosphate glucose, UDPG) is a nucleotide sugar. It is used in nucleotide sugar metabolism as an activated form of glucose, a substrate for enzymes called glucosyltransferases. [1] Uridine diphosphate glucose has been shown to have tissue-specific effects that have proved to be of clinical value in the treatment of some liver ailments. It is also known to have multiple effects on intrahepatic bilirubin metabolism which, in turn, are related to the glycogen synthesis occurring in the liver.[2]
In vitro study demonstrated that the effects of UDPG on cell metabolism do not appear to be limited to enzyme induction. Others have reported that UDPG can have effects under conditions that bar enzyme induction. Results showed that a significant amount of the UDPG, even though it is a highly polar compound, does pass through the membrane unchanged. A large fraction of the UDPG added to incubation media, however, was found in the cell as glucose phosphate, indicating cleavage after penetration of the cell. Eventually. all the UDPG that entered the cells was degraded to glucose phosphate and glucose. The in vitro studies show that G-6-P is not the active form, and several tests show that uridine does not lead to changes like those seen with UDPG. [2]
In vivo study indicated that indicate that the intracellular level of PRPP in animal tissues is greatly affected by extracellular UDPG. The alteration of PRPP level by UDPG is not linearly dose-related. The changes in PRPP that were induced by UDPG were also tissue-specific: mouse liver was more sensitive than was the spleen. This latter specificity may well be related to the therapeutically beneficial effects of UDPG.[2]
References:
[1]. Rademacher T, Pet al. "Glycobiology". Annu Rev Biochem. 1988; 57: 785–838.
[2]. Yip LC, et al. Effects of uridine diphosphoglucose (UDPG) infusion on 5-phosphoribosyl pyrophosphate (PRPP) levels of mouse tissues. Biochem Pharmacol. 1987 Mar 1;36(5):633-7.
尿苷二磷酸葡萄糖（尿嘧啶二磷酸葡萄糖，UDPG）是一种核苷酸糖。它作为葡萄糖的活化形式用于核苷酸糖代谢，葡萄糖是称为葡糖基转移酶的酶的底物。 [1] 尿苷二磷酸葡萄糖已被证明具有组织特异性作用，已证明在某些肝脏疾病的治疗中具有临床价值。还已知它对肝内胆红素代谢有多种影响，而后者又与肝脏中发生的糖原合成有关。[2]
体外研究表明，UDPG 对细胞代谢的影响似乎并不局限于酶诱导。其他人报告说，UDPG 可以在禁止酶诱导的条件下发挥作用。结果表明，大量的 UDPG，即使它是一种高极性化合物，也会通过膜而不会发生变化。然而，在细胞中发现加入孵育培养基的大部分 UDPG 为磷酸葡萄糖，表明在穿透细胞后发生裂解。最终。所有进入细胞的UDPG都被降解为磷酸葡萄糖和葡萄糖。体外研究表明 G-6-P 不是活性形式，多项测试表明尿苷不会导致像 UDPG 那样的变化。 [2]
体内研究表明，动物组织中 PRPP 的细胞内水平受细胞外 UDPG 的影响很大。 UDPG 对 PRPP 水平的改变不是线性剂量相关的。 UDPG 诱导的 PRPP 变化也是组织特异性的:小鼠肝脏比脾脏更敏感。后一种特异性很可能与 UDPG 的治疗有益作用有关。[2]
| Kinase experiment [1]: | |
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Preparation Method |
The reaction mixture for 20S proteasome inhibitory assay contained 0.1 M Tris-acetate, pH 7.0, 20S proteasome, MG-132 and 25 μM substrate dissolved in DMSO in a final volume of 1 ml. |
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Reaction Conditions |
After incubation at 37 ℃ for 15 min, the reaction was stopped by the addition of 0.1 ml of 10% SDS and 0.9 ml of 0.1 M Tris-acetate, pH 9.0. |
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Applications |
After measurement of fluorescence of reaction products, the IC50 of MG-132 against m-calpain and 20S proteasome can be determined. MG-132 inhibits 20S proteasome with IC50 of 100 nM. |
| Cell experiment [2]: | |
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Cell lines |
KIM-2 |
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Preparation Method |
MG-132 were diluted in Me2SO. Cells were treated with protease inhibitors or dilutant alone. Supernatant and monolayer cells were harvested by centrifugation and fixed in 70% ethanol in PBS for staining with acridine orange. Equal volumes of cells and acridine orange (5 mg/ml in PBS) were mixed on a microscope slide and examined by fluorescence microscopy. |
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Reaction Conditions |
0, 1.5, 5 μM, 24 h |
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Applications |
MG-132 treatment induces apoptosis in a cell cycle dependent manner. |
| Animal experiment [2]: | |
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Animal models |
C57BL/10ScSn DMD mdx mice |
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Preparation Method |
Localized administration was performed by injection of MG-132 into the gastrocnemius muscles of mdx mice. To visualize the injected muscle, MG-132 (final concentration of 20 μmol/L) was pre-mixed with 1% India ink in phosphate-buffered saline (PBS) for a total volume of 100 μl. Mice were sacrificed 24 hours after injection, and skeletal muscles were quickly isolated for further analysis. To systemically administer MG-132, Alzet Minipumps was subcutaneously implanted in the anterior back region of mdx mice. Experiments were conducted on 6-month-old mdx mice. For 8 days, administration of either different concentrations of MG-132 (delivered at rate of either 1 μg, or 5 μg or 10 μg/kg/24 hours) or the inhibitor-diluent (PBS only) was enforced, as a negative control. Skeletal muscle tissues were collected from untreated (PBS only) and MG-132-treated mdx mice for further analysis. |
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Dosage form |
1 μg, 5 μg, 10 μg/kg, injection into the gastrocnemius muscles or subcutaneously implanted Alzet Minipumps |
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Applications |
MG-132, as a proteasomal inhibitor, effectively rescues the expression levels and plasma membrane localization of dystrophin, β-dystroglycan, α-dystroglycan, and α-sarcoglycan in skeletal muscle fibers from mdx mice. Furthermore, MG-132 reduces muscle membrane damage, as revealed by vital staining of the diaphragm and gastrocnemius muscle isolated from treated mdx mice, and ameliorates the histopathological signs of muscular dystrophy, as judged by hematoxylin and eosin staining of muscle biopsies taken from treated mdx mice. |
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References: [1]. Tsubuki, S et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. Journal of biochemistry vol. 119,3 (1996): 572-6. [2]. MacLaren, A P et al. p53-dependent apoptosis induced by proteasome inhibition in mammary epithelial cells. Cell death and differentiation vol. 8,3 (2001): 210-8. [3]. Bonuccelli, Gloria et al. Proteasome inhibitor (MG-132) treatment of mdx mice rescues the expression and membrane localization of dystrophin and dystrophin-associated proteins. The American journal of pathology vol. 163,4 (2003): 1663-75. |
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| Cas No. | 133-89-1 | SDF | |
| 别名 | UDP-葡萄糖 | ||
| Canonical SMILES | OC[C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)OP(OP(OC[C@@H]2O[C@@H](N3C=CC(NC3=O)=O)[C@H](O)[C@@H]2O)(O)=O)(O)=O)O)O)O | ||
| 分子式 | C15H24N2O17P2 | 分子量 | 566.3 |
| 溶解度 | Water : ≥ 50 mg/mL | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| 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 | 1.7658 mL | 8.8292 mL | 17.6585 mL |
| 5 mM | 0.3532 mL | 1.7658 mL | 3.5317 mL |
| 10 mM | 0.1766 mL | 0.8829 mL | 1.7658 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet