苦龙胆酯苷|T5497|TargetMol

AMAROGENTIN
21018-84-8

￥169 1mg 起订

￥236 2mg 起订

￥376 5mg 起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 苦龙胆酯苷

英文名称：: AMAROGENTIN

CAS号：: 21018-84-8

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥95%

产品类别：: 抑制剂

货号：: T5497

Product Introduction

Bioactivity

Name	AMAROGENTIN
Description	Amarogentin is mainly extracted from Swertia and Gentiana roots. It plays cemopreventive/therapeutic role during liver carcinogenesis through modulation of cell cycle and apoptosis
Kinase Assay	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].
In vivo	Amarogentin，一种来自S. chirayita的苦味secoiridoid glycoside，在多种病理生理条件下展现出不同的活性，主要在利什曼病和癌症生成中表现突出。实验分析揭示，Amarogentin通过下调cyclooxygenase-2 (COX-2)活性，有助于抑制小鼠模型中的皮肤癌生成；然而，对Amarogentin选择性抑制可诱导的cyclooxygenase (COX)亚型尚无报道[1]。Amarogentin抑制人类胃癌细胞SNU-16的生长（48小时后IC50 = 12.4μM），当浓度达到50μM时增加细胞凋亡。Amarogentin（10-50 mg/kg，s.c.）在SNU-16裸鼠异种移植模型中剂量依赖性地减少肿瘤生长[2]。
Storage	keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 2 mg/mL (3.4 mM)
Keywords	Apoptosis \| AMPK \| AMP-activated protein kinase \| Inhibitor \| inhibit \| AMAROGENTIN
Inhibitors Related	Chitosan oligosaccharide \| Metronidazole \| 5-Fluorouracil \| Stavudine \| Tributyrin \| Dextran sulfate sodium salt (MW 4500-5500) \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Sodium 4-phenylbutyrate
Related Compound Libraries	Neuroprotective Compound Library \| Selected Plant-Sourced Compound Library \| Bioactive Compounds Library Max \| Anti-Tumor Natural Product Library \| Natural Product Library \| Traditional Chinese Medicine Monomer Library \| Antiparasitic Natural Product Library \| Terpene Natural Product Library \| Anti-Inflammatory Traditional Chinese Medicine Compound Library \| Saccharide and Glycoside Natural Product Library

苦杏苷|||苦龙胆酯苷|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子