價格 | ¥169 | ¥236 | ¥376 |
包裝 | 1mg | 2mg | 5mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-02 |
中文名稱:苦龍膽酯苷 | 英文名稱:AMAROGENTIN |
CAS:21018-84-8 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: ≥95% | 產(chǎn)品類別: 抑制劑 |
貨號: T5497 |
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,一種來自S. chirayita的苦味secoiridoid glycoside,在多種病理生理條件下展現(xiàn)出不同的活性,主要在利什曼病和癌癥生成中表現(xiàn)突出。實驗分析揭示,Amarogentin通過下調(diào)cyclooxygenase-2 (COX-2)活性,有助于抑制小鼠模型中的皮膚癌生成;然而,對Amarogentin選擇性抑制可誘導的cyclooxygenase (COX)亞型尚無報道[1]。Amarogentin抑制人類胃癌細胞SNU-16的生長(48小時后IC50 = 12.4μM),當濃度達到50μM時增加細胞凋亡。Amarogentin(10-50 mg/kg,s.c.)在SNU-16裸鼠異種移植模型中劑量依賴性地減少腫瘤生長[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) |
關鍵字 | Apoptosis | AMPK | AMP-activated protein kinase | Inhibitor | inhibit | AMAROGENTIN |
相關產(chǎn)品 | Chitosan oligosaccharide | L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate |
相關庫 | 神經(jīng)保護化合物庫 | 植物來源化合物庫 | 已知活性化合物庫 | 抗癌天然產(chǎn)物庫 | 天然產(chǎn)物庫 | 中藥單體化合物庫 | 抗寄生蟲天然產(chǎn)物庫 | 萜類天然產(chǎn)物庫 | 中藥抗炎分子庫 | 糖類及苷類化合物庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.2651萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 化學試劑,生物活性小分子 | 經(jīng)營模式 | 貿(mào)易,試劑,定制,服務 |
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