您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Darbufelone
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Darbufelone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Darbufelone图片
CAS NO:139226-28-1
包装:1mg
市场价:2000元

产品名称
CI-1004
产品介绍
Darbufelone 是细胞PGFLTB4产生的双重抑制剂。Darbufelone 有效抑制PGHS-2(IC50=0.19 μM),但对PGHS-1效力要低得多 (IC50=20 μM)。
生物活性

Darbufelone is a dual inhibitor of cellularPGFandLTB4production. Darbufelone potently inhibitsPGHS-2(IC50= 0.19 μM) but is much less potent withPGHS-1(IC50=20 μM).

IC50& Target

IC50: 0.19 μM (PGHS-2), 20 μM (PGHS-1)[1]

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 IC50of 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].

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].

分子量

332.46

性状

Solid

Formula

C18H24N2O2S

CAS 号

139226-28-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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