Atraric acid NEW
| Price | $41 |
| Package | 500mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: Atraric acid | CAS No.: 4707-47-5 |
| Purity: 99.59% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | Atraric acid |
| 描述 | Atraric acid derivatives as a new chemical lead structure for novel therapeutic compounds as AR antagonists, that can be used for prophylaxis or treatment of prostatic diseases. It inhibits PTP1B activity in a dose-dependent manner with IC50 values of 51.5 uM, suggest that atraric acid has potential to treat diabetes. |
| 體外活性 | Androgen receptor (AR) antagonists are important compounds for the treatment of prostate cancer (PCa). The Atraric acid (AA), a natural compound, binds to the AR and acts as a specific AR antagonist. Interestingly, Atraric acid represents a novel chemical platform that could serve as a potential basis for new AR antagonists. METHODS AND RESULTS:Therefore, one objective of this study was to analyze the chemical/structural requirements for AR antagonism and to obtain predictions of where and how Atraric acid binds to the AR. Further, this study describes the chemical synthesis of 12 Atraric acid derivatives and their analysis using a combination of computational and functional assays. Functional analysis of Atraric acid derivatives indicated that none activated the AR. Both the para-hydroxyl group and the benzene ortho- and the meta-methyl groups of Atraric acid appeared to be essential to antagonize androgen-activated AR activity. Furthermore, extension of the hydrophobic side chain of Atraric acid led to slightly stronger AR antagonism. In silico data suggest that modifications to the basic Atraric acid structure change the hydrogen-bonding network with the AR ligand binding domain (LBD), so that the para-hydroxyl group of Atraric acid forms a hydrogen bond with the LBD, confirming the functional importance of this group for AR antagonism. Moreover, in silico modeling also suggested that the ortho- and meta- methyl groups of Atraric acid interact with hydrophobic residues of the ligand pocket of AR, which might explain their functional importance for antagonism. CONCLUSIONS:Thus, these studies identify the chemical groups of Atraric acid that play key roles in allowing the Atraric acid-based chemical platform to act as an AR antagonist. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 13 mg/mL (66.26 mM) |
| 關(guān)鍵字 | Atraric acid |
| 相關(guān)產(chǎn)品 | β-Glycerophosphate disodium salt pentahydrate | Tartaric acid disodium dihydrate | Cyclosporine | Stearic acid | Flutamide |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 中藥單體化合物庫(kù) | 植物來(lái)源化合物庫(kù) | 天然產(chǎn)物庫(kù) | 抑制劑庫(kù) | 神經(jīng)保護(hù)化合物庫(kù) | 高通量篩選天然產(chǎn)物庫(kù) | 已知活性化合物庫(kù) | 藥食同源庫(kù) |
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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