楝酰胺|TQ0131|TargetMol

Rocaglamide
84573-16-0

￥1799 1mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

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邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 楝酰胺

英文名称：: Rocaglamide

CAS号：: 84573-16-0

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.46%

产品类别：: 抑制剂

货号：: TQ0131

Product Introduction

Bioactivity

名称	Rocaglamide
描述	Rocaglamide (Roc-A), isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-κB activation in T-cells.
细胞实验	HepG2 and Huh-7 cells (1×10^4/well) are seeded in 96-well plates in complete culture medium and incubated for 24 h. The cells are then exposed to 100 nM Rocaglamide and/or 100 ng/mL TRAIL for 24 h. The control cells are treated with DMSO at a concentration equal to that used for the drug-treated cells. The complete culture medium is then removed and MTT (200 μL, 0.5 mg/mL in 10% FBS-containing DMEM) is added to each well and the plate is incubated for 2 h at 37°C in a humidified incubator. The solution is then removed from the wells and 200 μL DMSO is added to each well prior to agitation. The absorbance at 570 nm is read using a microplate reader (Bio-Tek ELx800). The value for the vehicle-treated cells is considered to indicate 100% viability. Furthermore, a crystal violet assay is carried out. Briefly, the cells (1×10^5/mL) are seeded in a 12 well plate for 12 h and treated with TRAIL (0-100 ng/mL) and/or RocA(1-100 nM) for 12 h. The treated cells are washed with phosphate-buffered saline (PBS), fixed with 4% paraformaldehyde for 15 min, and stained using crystal violet for a further 30 min [2].
动物实验	The Huh-7 cells (3×10^6), suspended in 100 μL mix (equal volumes of DMEM and Matrigel), are implanted subcutaneously into the right flank of 10 female SCID mice (6-week-old) and then randomly divided into two equal groups, one of which received an intraperitoneal injection of Rocaglamide (2.5 mg/kg in 80 μL olive oil; n=5) and the other, used as a vehicle control, received olive oil alone (n=5). These treatments are performed once daily for 32 days and the tumor volumes and body weights of the animals are measured twice a week. The tumor volumes (mm3) are calculated using the following formula: Tumor volume=LS2/2, where L is the longest diameter and S is the shortest. At the end of the experiments, the mice are sacrificed and tumor samples are harvested, fixed in formalin and embedded in paraffin as tissue sections for immunohistochemical analysis [2].
体外活性	Rocaglamide是一种有效且选择性的热休克因子1（HSF1）激活抑制剂，IC50约为50 nM。它通过抑制转录启动因子eIF4A的功能发挥作用，并且具有针对白血病[1,2,3]的抗癌特性。单独使用Rocaglamide可导致9%的HepG2细胞和11%的Huh-7细胞发生凋亡，而与TRAIL联合治疗则分别使16%的HepG2细胞和17%的Huh-7细胞发生凋亡。然而，Rocaglamide与TRAIL的组合使用在HepG2和Huh-7细胞中引发的凋亡率分别高达55%和57%，明显超出了简单加成效应[2]。
体内活性	在Rocaglamide处理组中，肿瘤体积与对照组相比为45±12%。Rocaglamide显著抑制肿瘤生长，与对照组相比有明显差异。使用Rocaglamide治疗期间，小鼠体重没有减少，且未观察到明显的毒性迹象[2]。
存储条件	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 10 mg/mL (19.78 mM) Ethanol : 5 mg/mL (9.89 mM)
关键字	NF-κB \| Rocaglamide \| Nuclear factor-kappaB \| Heat shock proteins \| inhibit \| Eukaryotic Initiation Factor (eIF) \| Nuclear factor-κB \| HSP \| Inhibitor
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楝酰胺|||Rocaglamide A|||Roc-A|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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