Darbufelone mesylate - CAS:139340-56-0

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Darbufelone mesylate (Synonyms:CI-1004 mesylate)

目录号 : KM6301 CAS No. : 139340-56-0 纯度 : 98%

Data Sheet 产品使用指南

Darbufelone mesylate (CI-1004 mesylate) 双重抑制细胞 PGF_2α 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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10mg		In-stock
25mg		In-stock
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500mg	询价	In-stock

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生物活性

Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF_2α and LTB₄ production. Darbufelone potently inhibits PGHS-2 (IC₅₀ = 0.19 μM) but is much less potent with PGHS-1 (IC₅₀= 20 μM).

体外研究

Darbufelone is a noncompetitive inhibitor of PGHS-2 (K_i=10±5 μM). Darbufelone quenches the fluorescence of PGHS-2 at 325 nm (lambda(ex)=280 nm) with K_d=0.98±0.03 μM.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) .

体内研究

Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis. 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.

分子式

C₁₈H₂₄N₂O₂S^.CH₄O₃S

分子量

428.57

CAS号

139340-56-0

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, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 110 mg/mL (256.67 mM; Need ultrasonic)

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
10 mM	0.2333 mL	1.1667 mL	2.3333 mL

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 (protect from 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。

In Vivo:

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

1.

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); Suspended solution; Need ultrasonic

此方案可获得 5.5 mg/mL (12.83 mM) 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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。