AMAROGENTIN NEW
Price | $33 | $52 | $81 |
Package | 2mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-17 |
Product Details
Product Name: AMAROGENTIN | CAS No.: 21018-84-8 |
Purity: ≥95% | Supply Ability: 10g |
Release date: 2024/11/17 |
Product Introduction
Bioactivity
名稱 | AMAROGENTIN |
描述 | Amarogentin is mainly extracted from Swertia and Gentiana roots. It plays cemopreventive/therapeutic role during liver carcinogenesis through modulation of cell cycle and apoptosis |
激酶實驗 | The computer-aided drug discovery methods were used to unravel the COX-2 inhibitory mechanism of Amarogentin and to check its selectivity for the inducible isoform over the constitutive one.?The generated theoretical models of both isoforms were subjected to molecular docking analysis with Amarogentin and twenty-one other Food and Drug Authority (FDA) approved lead molecules.?The post-docking binding energy profile of Amarogentin was comparable to the binding energy profiles of the FDA approved selective COX-2 inhibitors.?Subsequent molecular dynamics simulation analysis delineated the difference in the stability of both complexes, with Amarogentin-COX-2 complex being more stable after 40ns simulation.?The total binding free energy calculated by MMGBSA for the Amarogentin-COX-2 complex was -52.35 KCal/mol against a binding free energy of -8.57 KCal/mol for Amarogentin-COX-1 complex, suggesting a possible selective inhibition of the COX-2 protein by the natural inhibitor.?Amarogentin achieves this potential selectivity by small, yet significant, structural differences inherent to the binding cavities of the two isoforms.?Hypothetically, it might block the entry of the natural substrates in the hydrophobic binding channel of the COX-2, inhibiting the cyclooxygenation step[1]. |
體內(nèi)活性 | Amarogentin, a bitter secoiridoid glycoside from S. chirayita, shows varied activity in several patho-physiological conditions, predominantly in leishmaniasis and carcinogenesis.?Experimental analysis has revealed that Amarogentin downregulates the cyclooxygenase-2 (COX-2) activity and helps to curtail skin carcinogenesis in mouse models;?however, there exists no account on selective inhibition of the inducible cyclooxygenase (COX) isoform by Amarogentin[1].marogentin inhibits the growth of SNU-16 human gastric cancer cells (IC50 = 12.4 μM after 48 hours) and increases apoptosis when used at a concentration of 50 μM. Amarogentin (10-50 mg/kg, s.c.) dose-dependently reduces tumor growth in a SNU-16 nude mouse xenograft model[2]. |
存儲條件 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 2 mg/mL (3.4 mM) |
關(guān)鍵字 | Apoptosis | AMPK | AMP-activated protein kinase | Inhibitor | inhibit | AMAROGENTIN |
相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Chitosan oligosaccharide |
相關(guān)庫 | 抗癌天然產(chǎn)物庫 | 萜類天然產(chǎn)物庫 | 經(jīng)典已知活性庫 | 中藥單體化合物庫 | 植物來源化合物庫 | 糖類及苷類化合物庫 | 抗寄生蟲天然產(chǎn)物庫 | 神經(jīng)保護化合物庫 | 抗衰老化合物庫 | 抗癌活性化合物庫 |
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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