Darbufelone mesylate NEW
| Price | $122 | $455 | Get Latest Price |
| Package | 5mg | 25mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-20 |
Product Details
| Product Name: Darbufelone mesylate | CAS No.: 139340-56-0 |
| Purity: 96.81% | Supply Ability: 10g |
| Release date: 2024/11/20 |
Product Introduction
Bioactivity
| Name | Darbufelone mesylate |
| Description | Darbufelone mesylate (CI-1004 mesylate) inhibited PGF2α and LTB4 in cells and demonstrated IC50 values of 0.19 μM for PGHS-2 and 20 μM for PGHS-1. |
| In vitro | Darbufelone, a noncompetitive inhibitor of PGHS-2 with a Ki value of 10±5 μM, exhibits fluorescence quenching of PGHS-2 at 325 nm (λex=280 nm) with a Kd of 0.98±0.03 μM[2]. To assess the putative anti-proliferative effect of Darbufelone, A549, H520, and H460 cell lines derived from three distinct pathological subtypes of non-small cell lung cancer (NSCLC) (adenocarcinoma, squamous, and large cell lung cancer, respectively) are utilized. The cell lines are treated with increasing concentrations of Darbufelone, ranging from 5 to 60 μM, for a duration of 72 hours. The growth inhibition of these three cell lines gradually increases with higher concentrations of the drug. The IC50 values for A549 and H520 are 20±3.6 and 21±1.8 μM, respectively, while H460 exhibits a lower IC50 of 15±2.7 μM[1]. |
| In vivo | Darbufelone, a dual inhibitor of cellular PGF2R and LTB4 production, exhibits oral activity in animal models of inflammation and arthritis without causing ulcers. When mice were treated with bufafenone at a dose of 80 mg/kg/day, the tumor volume decreased in a time-dependent manner. In contrast, lower doses of bufafenone (20 or 40 mg/kg/day) did not significantly inhibit tumor weight. At necropsy, the tumor weight of mice treated with bufafenone (80 mg/kg/day) was reduced by 30.2% compared to the control group. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 100 mg/mL (233.33 mM), Sonication is recommended. H2O : <0.1 mg/mL |
| Keywords | CI 1004 Mesylate | Darbufelone Mesylate | CI1004 Mesylate | CI-1004 Mesylate |
| Inhibitors Related | Montelukast sodium | Tranilast | Rutin | Rebamipide |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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