1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. COX Endogenous Metabolite
  3. Valdecoxib

Valdecoxib  (Synonyms: 伐地考昔; SC 65872)

目录号: HY-15762 纯度: 99.90%
COA 产品使用指南

Valdecoxib 是一种高效的,可口服的,选择性的 COX-2 抑制剂,对 COX-2COX-1IC50 值分别为 5 nM 和 140 μM,可用于关节炎和疼痛的研究。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Valdecoxib Chemical Structure

Valdecoxib Chemical Structure

CAS No. : 181695-72-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥900
In-stock
5 mg ¥511
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10 mg ¥818
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25 mg ¥1636
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50 mg ¥2617
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100 mg ¥4188
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200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of Valdecoxib:

查看 COX 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.

IC50 & Target[1]

COX-2

5 nM (IC50)

COX-1

140 μM (IC50)

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Valdecoxib (Compound 2) is a highly potent, selective and orally active inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively[1]. Valdecoxib (10, 100 µM) inhibits LPS-induced proliferation of endothelial cells and bFGF secretion in a dose-dependent manner. Valdecoxib stimulates VEGF formation via HMEC-1 under inflammatory conditions[2].

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

体内研究
(In Vivo)

Valdecoxib (Compound 2) shows potent oral activity in an acute antiinflammatory assay (rat carrageenan foot pad edema; ED50 = 10.2 ± 1.4 mg/kg). Valdecoxib also has chronic antiinflammatory activity in the rat adjuvant arthritis model, with an ED50 of 0.032 ± 0.002 mg/kg/day[1]. Valdecoxib (10 mg/kg, i.p.) significantly attenuates the behavioral and biochemical (oxidative damage) alterations in chronic-stressed mice[3].

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

Clinical Trial
分子量

314.36

Formula

C16H14N2O3S

CAS 号
性状

固体

颜色

White to off-white

中文名称

伐地昔布

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 34 mg/mL (108.16 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)

* "≥" 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 3.1811 mL 15.9053 mL 31.8107 mL
5 mM 0.6362 mL 3.1811 mL 6.3621 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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 (7.95 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 (7.95 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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.90%

参考文献
Cell Assay
[2]

HMEC-1 cells proliferation is measured using the MTT conversion method. Cells are seeded (50.000 cells/well) into 96-well plates. The cells are incubated for 24 h with LPS 100 µg/mL, CoCl2 200 µM, Valdecoxib 10 or 100 µM, LPS and Valdecoxib or CoCl2 and Valdecoxib or without tested chemicals (control group). All the substances are added at the same time. After incubation, 50 µL MTT (1 mg/mL) is added and the plates are incubated at 37°C for 4 h. At the end of the experiment, cells are exposed to 100 µL DMSO, which enables the release of the blue reaction product-formazan. The absorbance at 570 nm is read on a microplate reader and results are expressed as a percentage of the absorbance measured in control cells[2].

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

Animal Administration
[3]

Mice[3]
The drugs including naproxen (14 mg/kg, i.p.), rofecoxib (5 mg/kg, i.p.), meloxicam (5 mg/kg, i.p.), nimesulide (5 mg/kg, i.p.) and Valdecoxib (10 mg/kg, i.p.) are used in the assay. The animals are randomized into 7 groups (n=10 in each group), including the naive group, in which the mice only receive vehicle for 15 d without forced swimming session; the control (chronically stressed) group, in which mice receive vehicle 30 min before the forced swimming session (6 min) for 15 d; the naproxen (14 mg/kg) group; the Valdecoxib (10 mg/kg) group; the rofecoxib (5 mg/kg) group; the meloxicam (5 mg/kg) group; and the nimesulide (5 mg/kg) group. Drugs are suspended in 0.25% carboxymethylcellulose (CMC) and administered intraperitoneally, 30 min before the forced swimming session for 15 consecutive days[3].

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

参考文献

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1811 mL 15.9053 mL 31.8107 mL 79.5267 mL
5 mM 0.6362 mL 3.1811 mL 6.3621 mL 15.9053 mL
10 mM 0.3181 mL 1.5905 mL 3.1811 mL 7.9527 mL
15 mM 0.2121 mL 1.0604 mL 2.1207 mL 5.3018 mL
20 mM 0.1591 mL 0.7953 mL 1.5905 mL 3.9763 mL
25 mM 0.1272 mL 0.6362 mL 1.2724 mL 3.1811 mL
30 mM 0.1060 mL 0.5302 mL 1.0604 mL 2.6509 mL
40 mM 0.0795 mL 0.3976 mL 0.7953 mL 1.9882 mL
50 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5905 mL
60 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3254 mL
80 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9941 mL
100 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.7953 mL
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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目录号:
HY-15762
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