2. GPCR/G Protein
  3. Prostaglandin Receptor Leukotriene Receptor
  4. Darbufelone mesylate

Darbufelone mesylate  (Synonyms: CI-1004 mesylate)

目录号: HY-101438A 纯度: 99.65%
COA 产品使用指南

摩尔计算器

Darbufelone mesylate (CI-1004 mesylate) 双重抑制细胞 PGF2α 和 LTB4 产生。Darbufelone 有效抑制 PGHS-2 (IC50=0.19 μM)，但对 PGHS-1 效力要低得多 (IC50=20 μM)。

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Darbufelone mesylate Chemical Structure

Darbufelone mesylate Chemical Structure

CAS No. : 139340-56-0

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Other Forms of Darbufelone mesylate:

Darbufelone mesylate 相关抗体

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).

IC50 & Target[1]

PGF2α

 

LTB4

 

PGHS-2

0.19 μM (IC50)

PGHS-1

20 μM (IC50)

体外研究
(In Vitro)

Darbufelone is a noncompetitive inhibitor of PGHS-2 (Ki=10±5 μM). Darbufelone quenches the fluorescence of PGHS-2 at 325 nm (lambda(ex)=280 nm) with Kd=0.98±0.03 μM[1].To test the putative anti-proliferative effect of Darbufelone, A549, H520 and H460 cell lines are used, which are established from three distinct pathological subtypes of NSCLC (adenocarcinoma, squamous and large cell lung cancer respectively). Increasing concentrations of Darbufelone, ranging from 5 to 60 μM, are tested for 72 h. The cell growth inhibition of these three cell lines gradually increases with higher drug concentration. The IC50 of A549 and H520 are 20±3.6 and 21±1.8 μM, respectively, while the H460 has much lower IC50 (15±2.7 μM) [2].

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

Darbufelone mesylate 相关抗体:
体内研究
(In Vivo)

Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis[1]. When mice are treated with Darbufelone at dosage of 80 mg/kg/day, the tumor volumes decrease in a time-dependent manner. In contrast, lower dose of Darbufelone (20 or 40 mg/kg/day) dos not show any significant inhibition of tumor weight. At necropsy, the tumor weight in mice treated with Darbufelone (80 mg/kg/day) is reduced by 30.2% in comparison with control group[2].

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

428.57

Formula

C19H28N2O5S2
CAS 号
性状

固体

颜色

White to light yellow

中文名称

甲磺酸达布非隆
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 110 mg/mL (256.67 mM; 超声助溶; 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 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3333 mL 11.6667 mL 23.3334 mL
5 mM 0.4667 mL 2.3333 mL 4.6667 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 (sealed storage, away from moisture and light)。-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。

  • 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: 5.5 mg/mL (12.83 mM); 悬浊液; 超声助溶

    此方案可获得 5.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 55.0 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。
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

只
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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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
参考文献
Kinase Assay
[1]

The effect of Darbufelone on the cyclooxygenase activity of PGHS-2 is determined in assays with no enzyme-inhibitor preincubation. HoloPGHS-2 (30 nM final concentration) is added to reaction mixtures that contain 20 mM Tris-HCl buffer (pH 7.4), 100 μM TMPD, and varying levels of Arachidonic acid (0-60 μM) and Darbufelone (0-30 μM). The cyclooxygenase activity is measured by monitoring the oxidation of TMPD at 610 nm using a microplate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

A549 (CCL-185, lung adenocarcinoma cancer cell line), NCI-H520 (HTB-182, lung squamous cancer cell line) and NCI-H460 (HTB-177, lung large cell cancer cell line) cells are cultured in RPMI-1640, supplemented with 10% (v/v) heat-inactivated fetal bovine serum, 2 mM L-glutamine, 100 U/mL Penicillin G, and 100μg/mL Streptomycin. Cells are grown at 37°C in a humidified atmosphere of 95% air and 5% CO2 and routinely passaged using 0.25% trypsin–EDTA. The effect of Darbufelone on human lung carcinoma cell viability is determined by MTT reduction assay. In brief, tumor cells growing in log-phase are trypsinized and seeded at 5×103 cells per well into 96-well plates and allowed to attach overnight. Medium in each well is replaced with fresh medium or medium containing various concentrations of Darbufelone (5-60 μM) in at least triplicate wells. Cells are cultured to another 72 h. After treatment, 1/10 volume of MTT solution (5 mg/mL) is added to each well, and the plate is incubated at 37°C for another 4 h. Two hundred microliters of DMSO is added to each well to solubilize the MTT-formazan product after removal of the medium. Absorbance at 595 nm is measured with a multi-well spectrophotometer. Growth inhibition is calculated as a percentage of the untreated controls[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
C57Bl/6 male mice at 4-5 weeks are used. These mice are housed in air-conditioned quarters and are provided food and water ad libitum. On the day 0, Lewis Lung Carcinoma cells (1×106) are implanted into the left armpit of C57Bl/6 mice. The mice are randomly divided into four treatment groups of ten animals each. The day after inoculation (day 1), control group is treated with CMC-Na, and other groups are administered Darbufelone by gavage at doses of 20, 40, and 80 mg/kg/day. The treatment is continued till the end of the study. On day 14, animals are killed, and tumors are excised, weighed, and fixed in formalin for the further histochemical analysis.

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

Darbufelone mesylate 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 (sealed storage, away from moisture and light)。-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
DMSO 1 mM 2.3333 mL 11.6667 mL 23.3334 mL 58.3335 mL
5 mM 0.4667 mL 2.3333 mL 4.6667 mL 11.6667 mL
10 mM 0.2333 mL 1.1667 mL 2.3333 mL 5.8334 mL
15 mM 0.1556 mL 0.7778 mL 1.5556 mL 3.8889 mL
20 mM 0.1167 mL 0.5833 mL 1.1667 mL 2.9167 mL
25 mM 0.0933 mL 0.4667 mL 0.9333 mL 2.3333 mL
30 mM 0.0778 mL 0.3889 mL 0.7778 mL 1.9445 mL
40 mM 0.0583 mL 0.2917 mL 0.5833 mL 1.4583 mL
50 mM 0.0467 mL 0.2333 mL 0.4667 mL 1.1667 mL
60 mM 0.0389 mL 0.1944 mL 0.3889 mL 0.9722 mL
80 mM 0.0292 mL 0.1458 mL 0.2917 mL 0.7292 mL
100 mM 0.0233 mL 0.1167 mL 0.2333 mL 0.5833 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.

Keywords:

Darbufelone139340-56-0CI-1004甲磺酸达布非隆CI1004CI 1004Prostaglandin ReceptorLeukotriene ReceptorInhibitorinhibitorinhibit

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