型号:
产品价格:电议      采购度:1598      原产地:美洲
发布时间:2021/7/23 22:11:40 所属地区:上海 上海市
简要描述:
Darbufelone mesylate (CI-1004 mesylate) 双重抑制细胞 PGF2α 和 LTB4 产生。Darbufelone 有效抑制 PGHS-2 (IC50= μM),但对 PGHS-1 效力要低得多 (IC50=20 μM)。
产品详情
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。
CAS No. : 139340-56-0
MCE 站:Darbufelone mesylate
产品活性: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)。
研究领域:GPCR/G Protein
作用靶点:Prostaglandin Receptor | Leukotriene Receptor
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.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) .
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. 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.
相关产品:Prostaglandin E2 | Prostaglandin E1 | MK-571 sodium salt | Iloprost | Montelukast sodium | MK-886 | PF-04418948 | Tranilast | ONO-AE3-208 | Zafirlukast | AH 6809 | U-46619 | Latanoprost | Laropiprant | Rebamipide | Travoprost | RO1138452 | Ramatroban | p-Hydroxycinnamic acid | Bimatoprost | Pectolinarin | Pranlukast | Taprenepag | Dinoprost tromethamine salt | (+)-Cloprostenol | Dazoxiben | Evatanepag | L-798106 | Seratrodast | Nedocromil
品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物,我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物;
• 10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果;
• 专业团队跟踪*新的制药及生命科学研究进展,为您提供全球*新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。
更新时间:2024/1/2 10:14:29
留言咨询
温馨提示
1.遵守中华人民共和国有关法律、法规,尊重网上道德,承担一切因您的行为而直接或间接引起的法律责任。
2.请您真实的反映产品的情况,不要捏造、诬蔑、造谣。如对产品有任何疑问,也可以留言咨询。
3.未经本站同意,任何人不得利用本留言簿发布个人或团体的具有广告性质的信息或类似言论。
相关新闻
相关产品