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CAPE (咖啡酸苯乙酯) /Phenethyl caffeate {[allProObj[0].p_purity_real_show]}

货号:A158279 同义名: 咖啡酸苯乙酯 / Caffeic acid phenethyl ester;CAPE

Caffeic acid phenethyl ester, a natural product isolated and purified from the barks of Cinnamomum cassia Presl, is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.

Phenethyl caffeate 化学结构 CAS号:104594-70-9
Phenethyl caffeate 化学结构
CAS号:104594-70-9
Phenethyl caffeate 3D分子结构
CAS号:104594-70-9
Phenethyl caffeate 化学结构 CAS号:104594-70-9
Phenethyl caffeate 3D分子结构 CAS号:104594-70-9
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Phenethyl caffeate 纯度/质量文件 产品仅供科研

货号:A158279 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 NF-κB 其他靶点 纯度
PDTC ammonium 98%
QNZ ++++

NF-κB, IC50: 11 nM

99%+
Sodium 4-Aminosalicylate Dihydrate 98%
Sodium Salicylate 95%
Parthenolide p53 97% HPLC
JSH-23 +

NF-κB, IC50: 7.1 μM

98%
Phenethyl caffeate 98%
Andrographolide 98+%
Curcumin HDAC,Nrf2 98%
SC75741 +++

NF-κB, EC50: 200 nM

99%+
CBL0137 HCl ++

NF-κB, EC50: 0.47 μM

p53 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Phenethyl caffeate 生物活性

靶点
  • NF-κB

描述 NF-κB is a transcription factor with heterodimer or homodimer form of rel family proteins including RelA (p65), RelB, cRel, p50 and p52. Caffeic Acid Phenethyl Ester (CAPE) is an NF-κB inhibitor isolated from propolis. Treatment with CAPE at concentration ranging in 20-40μM for 2h could dose-dependently inhibit phosphorylation of IκBα and subsequently nuclear translocation of NF-κB (present as p65) induced by LPS in hepatic stellate cells. The increased nitrite production and the transcription and protein synthesis of MCP-1, IL-6 and iNOS induced by LPS could be significantly reduced by CAPE at concentration ranging in 5-40μM in a concentration-dependent manner in the same cells. Similarly, TNF-activated binding of NF-κB to DNA, phosphorylation of IκBα (within 30min) and p65 nuclear translocation could be observed in U937 cells pre-treated with 25μg/ml CAPE. Oral administration of 30mg/kg of CAPE daily for 4 weeks could improve the glucose sensitivity associated with the improvement in insulin-stimulated phosphorylation of the insulin receptor substrate-2 and an increase in Akt phosphorylation, promote amelioration in hepaticsteatosis, as well as reduced the induction of the inflammatory pathway, including JNK, NF-κB and COX-2 pathway, in high-fat-diet mice.

Phenethyl caffeate 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A549 cells Cytotoxic assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=26.8 μM 20673727
human BCG823 cells Cytotoxic assay Cytotoxicity against human BCG823 cells by MTT assay, IC50=44.6 μM 18952420
human Bel7402 cells Cytotoxic assay Cytotoxicity against human Bel7402 cells by MTT assay, IC50=5.5 μM 18952420
human Bel7404 cells Cytotoxic assay 72 h Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay, IC50=14.5 μM 20673727

Phenethyl caffeate 动物研究

Dose Rat: 3 mg/kg, 6 mg/kg[3] (i.p.); 1 mg/kg - 20 mg/kg[4] (i.v.); 20 μg/kg/day[5] (p.o.) Pups: 40 mg/kg[6] (i.p.)
Administration i.p., i.v., p.o.
Pharmacokinetics
Animal Rats[7]
Dose 20 mg/kg
Administration i.v.
CLt 148.2 ± 70.4 ml/min/kg
T1/2 28.7 ± 9.1 min
B 1.071 ± 0.926 μg/ml
α 0.468 ± 0.038 min-1
Vz 5784 ± 2579 min/kg
A 53.6 ± 15.6 μg/ml
AUC 160.5 ± 74.4 μg·min/ml
β 0.027 ± 0.011 min-1

Phenethyl caffeate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02744703 Matrix Metalloproteinase Inhib... 展开 >>itors Composite Resins 收起 << Not Applicable Completed - -

Phenethyl caffeate 参考文献

[1]Banskota AH, Nagaoka T, et al. Antiproliferative activity of the Netherlands propolis and its active principles in cancer cell lines. J Ethnopharmacol. 2002 Apr;80(1):67-73.

[2]Natarajan K, Singh S, et al. Caffeic acid phenethyl ester is a potent and specific inhibitor of activation of nuclear transcription factor NF-kappa B. Proc Natl Acad Sci U S A. 1996 Aug 20;93(17):9090-5.

[3]Kumar M, Kaur D, et al. Caffeic Acid Phenethyl Ester (CAPE) Prevents Development of STZ-ICV Induced dementia in Rats. Pharmacogn Mag. 2017 Jan;13(Suppl 1):S10-S15.

[4]Iraz M, Fadillioglu E, et al. Role of vagal activity on bradicardic and hypotensive effects of caffeic acid phenethyl ester (CAPE). Cardiovasc Toxicol. 2005 Fall;5(4):391-6.

[5]Bozkurt Y, Bozkurt M, et al. Caffeic acid phenethyl ester protects kidneys against acetylsalicylic acid toxicity in rats. Ren Fail. 2012;34(9):1150-5.

[6]Wei X, Zhao L, et al. Caffeic acid phenethyl ester prevents neonatal hypoxic-ischaemic brain injury. Brain. 2004 Dec;127(Pt 12):2629-35. Epub 2004 Oct 6.

[7]Wang X, Pang J, et al. Pharmacokinetics of caffeic acid phenethyl ester and its catechol-ring fluorinated derivative following intravenous administration to rats. Biopharm Drug Dispos. 2009 Jul;30(5):221-8.

Phenethyl caffeate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.59mL

3.52mL

1.76mL

35.17mL

7.03mL

3.52mL

Phenethyl caffeate 技术信息

CAS号104594-70-9
分子式C17H16O4
分子量 284.31
别名 咖啡酸苯乙酯 ;Caffeic acid phenethyl ester;CAPE;BAF-IN-C09;β-Phenylethyl Caffeate;2-Phenylethyl Caffeate;Caffeic Acid phenylethyl ester;Phenylethyl Caffeate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(369.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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