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Tetrahydrouridine dihydrate  (Synonyms: 四氢尿苷; THU dihydrate; NSC-112907 dihydrate)

目录号: HY-15345 纯度: 99.79%
COA 产品使用指南

Tetrahydrouridine dihydrate (THU dihydrate) 是一种有效的胞苷脱氨酶 (CDA) 抑制剂,竞争性阻断酶的活性位点。

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Tetrahydrouridine dihydrate Chemical Structure

Tetrahydrouridine dihydrate Chemical Structure

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1 mg ¥1300
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5 mg ¥3300
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10 mg ¥5400
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Customer Review

Other Forms of Tetrahydrouridine dihydrate:

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.

IC50 & Target

cytidine deaminase (CDA)[1]

体外研究
(In Vitro)

Tetrahydrouridine (THU) is a specific inhibitor of cytidine deaminase (CDA) which can suppress deamination in the catabolism of cytotoxic deoxycytidine analogues like ara-C and Gemcitabine. To test how Tetrahydrouridine affects the Gemcitabine-mediated anti-neoplastic effect on pancreatic and lung carcinoma cells, a combination therapy is performed. As expected, high CDA expression in BxPC-3 and H441 results in improved Gemcitabine sensitivity after a 100 μM Tetrahydrouridine treatment. The sensitivity of BxPC-3 and H441 cell lines increases by as much as approximately 2.1 and 4.4 fold respectively. On the other hand, MIAPaCa-2 and H1299 cells unexpectedly become more sensitive to Gemcitabine with low CDA expression. MIAPaCa-2 and H1299 cells show a change in IC50 of 2.2 and 2.3 fold respectively. However, Panc-1 and H322 cells do not show significant changes in drug sensitivity. These data suggested that Tetrahydrouridine can sensitize some pancreatic and lung carcinoma cells to Gemcitabine-induced cell death regardless of CDA expression levels. Tetrahydrouridine inhibits S-phase without apoptosis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Administration of 167 mg/kg Tetrahydrouridine (THU) followed by 1.0 mg/kg DAC results in death in one male and eight females. Animals surviving to scheduled termination are generally asymptomatic with no treatment related effects observed in body weights, food consumption, clinical chemistry and urinalysis for a treatment up to 1.0 mg/kg DAC in combination with 167 mg/kg Tetrahydrouridine in animals[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

284.26

Formula

C9H20N2O8

性状

固体

颜色

White to off-white

中文名称

四氢尿苷二水合物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (351.79 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 50 mg/mL (175.90 mM; 超声助溶)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5179 mL 17.5895 mL 35.1791 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.79 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.79 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.86%

参考文献
Cell Assay
[1]

Cell growth for pancreatic and lung carcinoma cell lines is carried out using the colorimetric methylene blue assay in 96-well plates at a density of 5,000 cells/well. Cells are either exposed or not exposed to Tetrahydrouridine (100 µM), counting the first 12 hrs as Day 0. Mean values are calculated from three different wells in triplicates for four days[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
CD-1 mice (male 30-38 g and female 24-31g) from are individually housed in polycarbonate cages suspended on stainless steel racks with SaniChip certified hardwood bedding. Mice are assigned to four dose groups and a vehicle control group. Animals are gavaged with DAC or its vehicle 1 hour ± 5 minutes after administration of THU or its vehicle at a dose volume of 10 mL/kg. The DAC doses are selected based on the range finding study in which the mice tolerated six oral doses (2x/week) of 0.1, 0.2 and 0.4 mg/kg DAC in combination with a fixed dose of 167 mg/kg THU. A fixed Tetrahydrouridine dose (500 mg/m2) and the optimal timing between Tetrahydrouridine and DAC administration (60 min) are selected. Conversion of milligrams per body surface area dose in mice into milligrams per kilogram body weight dose estimation is based on Michaelis constant (km) values for mice obtained from US Food and Drug Administration published guidelines. In brief, the mouse dose in milligrams per body surface area (500 mg/m2) is divided by the km of 3 to convert the dose to milligrams per kilogram body weight (167 mg/kg).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Tetrahydrouridine dihydrate 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.5179 mL 17.5895 mL 35.1791 mL 87.9477 mL
5 mM 0.7036 mL 3.5179 mL 7.0358 mL 17.5895 mL
10 mM 0.3518 mL 1.7590 mL 3.5179 mL 8.7948 mL
15 mM 0.2345 mL 1.1726 mL 2.3453 mL 5.8632 mL
20 mM 0.1759 mL 0.8795 mL 1.7590 mL 4.3974 mL
25 mM 0.1407 mL 0.7036 mL 1.4072 mL 3.5179 mL
30 mM 0.1173 mL 0.5863 mL 1.1726 mL 2.9316 mL
40 mM 0.0879 mL 0.4397 mL 0.8795 mL 2.1987 mL
50 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7590 mL
60 mM 0.0586 mL 0.2932 mL 0.5863 mL 1.4658 mL
80 mM 0.0440 mL 0.2199 mL 0.4397 mL 1.0993 mL
100 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8795 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Tetrahydrouridine dihydrate
目录号:
HY-15345
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