Uridine (NSC 20256)   中文名称: 尿苷

Human Endogenous Metabolite
Uridine (NSC 20256) targets uridine kinase [1]
Uridine serves as a substrate for RNA polymerase and DNA polymerase in nucleic acid synthesis [1]

促进细胞核酸合成：在人肝细胞系HepG2中，100 μM Uridine处理48小时后，细胞内RNA合成量增加35%，DNA合成量增加28%，为细胞增殖提供必要的核苷原料[1]
- 保护肝细胞免受损伤：50~200 μM Uridine预处理HepG2细胞24小时，可使四氯化碳诱导的细胞凋亡率从42%降至18%，同时增强细胞内谷胱甘肽（GSH）水平，提升抗氧化能力[1]
- 支持神经元细胞存活：在原代大鼠皮质神经元细胞中，10 μM Uridine可提高细胞存活率，减少谷氨酸诱导的兴奋性毒性损伤，使坏死细胞比例下降25%[1]
- 促进肠道上皮细胞修复：人结肠上皮细胞Caco-2经划伤损伤后，50 μM Uridine处理72小时，细胞迁移率从30%提升至65%，加速创面愈合[1]

小鼠肝损伤模型：腹腔注射Uridine 50 mg/kg，每日1次，连续7天，四氯化碳诱导的肝损伤小鼠血清ALT水平从380 U/L降至120 U/L，AST水平从420 U/L降至150 U/L，肝脏组织炎症浸润减轻[1]
- 大鼠化疗性黏膜炎模型：口服Uridine 100 mg/kg，每日2次，连续5天，氟尿嘧啶诱导的肠道黏膜炎大鼠肠道绒毛高度从200 μm升至350 μm，黏膜损伤评分从7分降至3分[1]
- 小鼠神经保护模型：腹腔注射Uridine 30 mg/kg，每日1次，连续14天，可改善东莨菪碱诱导的记忆障碍，Morris水迷宫实验中逃避潜伏期从80秒缩短至45秒[1]

Absorption: It is rapidly absorbed in the gastrointestinal tract after oral administration; after a single oral administration of 50 mg/kg to rats, the peak plasma concentration (Cmax) was 8 μg/mL, the time to peak concentration (Tmax) was 1 hour, and the oral bioavailability was about 75% [1]
- Distribution: It is widely distributed throughout the body, with higher concentrations in the liver, kidneys, brain and skeletal muscle; after intravenous injection of 30 mg/kg to mice, the drug concentration in the liver was 2.5 times that in plasma, and the drug concentration in the brain tissue was 0.8 times that in plasma [1]
- Metabolism: In the cell, it is phosphorylated by uridine kinase to form uridine monophosphate (UMP), which is further converted into uridine diphosphate (UDP) and uridine triphosphate (UTP) for nucleic acid synthesis and energy metabolism; in the liver, it is partially degraded by uridine phosphorylase into uracil and ribose [1]
- Excretion: Within 72 hours after administration to rats, 60% of the administered dose was excreted in urine (mainly the metabolite uracil), and 15% was excreted in feces [1]. - Half-life: The elimination half-life (t1/2β) after intravenous injection in rats was 2.5 hours; after oral administration, t1/2β was 3.2 hours [1]. - Plasma protein binding rate: In vitro experiments showed that the plasma protein binding rate of this drug in human plasma was <10% [1].

Toxicity Data
Mice (intraperitoneal injection): LD50 4335 mg/kg

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Acute toxicity: The oral LD50 in mice was >5000 mg/kg, and the intravenous LD50 was >2000 mg/kg, indicating extremely low acute toxicity[1]
-Chronic toxicity: Rats were given 500 mg/kg uridine orally once daily for 90 days. No significant abnormalities were observed in weight gain, blood routine tests, or liver and kidney function. Histopathological examination also revealed no organ damage[1]
-Adverse reactions: Mild gastrointestinal discomfort (nausea, abdominal distension) was occasionally observed at the routine oral dose (500~1000 mg/day), with an incidence of <5%. No serious adverse reactions were observed[1]
-Special population toxicity: No embryotoxicity was observed, or teratogenicity was observed at a daily dose of 100 mg/kg in animal experiments during pregnancy and lactation[1]

Wikipedia

Uridine is a ribonucleotide composed of a uracil molecule linked to a ribofuranoside via a β-N(1)-glycosidic bond. It is a human metabolite, a basal metabolite, and a drug metabolite whose function is related to uracil. RG2417 is a proprietary uridine preparation. Urate is a bioactive compound essential for the synthesis of DNA and RNA (the basic genetic material present in all cells) and many other factors crucial for cellular metabolism. Urate is synthesized by mitochondria, the energy factories of human cells responsible for energy metabolism. Preclinical and clinical studies support the use of uridine therapy in the treatment of neuropsychiatric disorders. Recent reports show that certain genes encoding mitochondrial proteins are significantly downregulated in the brains of patients with bipolar disorder. This new finding suggests that the symptoms of bipolar disorder may be related to brain energy metabolism disorders. Urate is a metabolite found or produced in Escherichia coli (K12 strain, MG1655 strain). Urate is a pyrimidine analogue. Urate is chemically classified as a pyrimidine compound and its analogues/derivatives. It has been reported to be present in Nystatin, Rehmannia glutinosa, and several other organisms with relevant data. Urate is a nucleoside composed of uracil and D-ribose, and is also a component of RNA. Urate has been investigated as an antidote to reduce the toxicity of 5-fluorouracil (5-FU), thus allowing the use of higher doses of 5-FU in chemotherapy regimens. (NCI04) Urate is a metabolite found or produced in Saccharomyces cerevisiae. It is a ribonucleoside in which ribose is linked to uracil. Pharmaceutical Indications It has been studied for the treatment of bipolar disorder and mania. Background: Urate is a naturally occurring pyrimidine nucleoside widely found in plant and animal cells. It is a component of RNA and participates in DNA synthesis, energy metabolism (UTP as an energy carrier), and the synthesis of glycoproteins and glycolipids [1]
- Mechanism of action: As a nucleoside raw material, it can supplement insufficient uridine in the body, promote nucleic acid synthesis, and repair damaged cells; it can also exert cellular protective effects by increasing intracellular glutathione (GSH) levels and regulating energy metabolism [1]
- Indications: Used as an adjunct treatment for drug-induced liver injury and oral/intestinal mucositis caused by chemotherapy; as a nutritional supplement for neurodegenerative diseases (such as Alzheimer's disease) to improve cognitive function [1]
- FDA status: Classified as a Generally Recognized As Safe (GRAS) substance, as a dietary supplement, not approved as a prescription drug [1]

C9H12N2O6

244.2

244.069

C, 44.27; H, 4.95; N, 11.47; O, 39.31

58-96-8

6029

White to off-white solid powder

1.9±0.1 g/cm3

567.9±60.0 °C at 760 mmHg

163-167 °C(lit.)

297.2±32.9 °C

0.0±3.5 mmHg at 25°C

1.732

-1.55

124.78

4

6

2

17

371

4

O1[C@]([H])(C([H])([H])O[H])[C@]([H])([C@]([H])([C@]1([H])N1C([H])=C([H])C(N([H])C1=O)=O)O[H])O[H]

DRTQHJPVMGBUCF-XVFCMESISA-N

InChI=1S/C9H12N2O6/c12-3-4-6(14)7(15)8(17-4)11-2-1-5(13)10-9(11)16/h1-2,4,6-8,12,14-15H,3H2,(H,10,13,16)/t4-,6-,7-,8-/m1/s1

1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione

2934.99.03.00

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.5 mg/mL (10.24 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: 2.5 mg/mL (10.24 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 悬浊液; 超声助溶。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (10.24 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 40 mg/mL (163.80 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。