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.
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产品名称 | NF-κB ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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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 | ✔ | Nrf2,HDAC | 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。 |
靶点 |
|
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. |
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 | |
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 |
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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 | - | - |
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 |
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 |