| 规格 | 价格 | 库存 | 数量 |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| 靶点 |
iNOS (inducible Nitric Oxide Synthase, IC50 = 25.6 μM for NO production inhibition) [1]
COX-2 (Cyclooxygenase-2, IC50 = 32.1 μM for PGE2 production inhibition) [1] |
|---|---|
| 体外研究 (In Vitro) |
在脂多糖(LPS,1 μg/mL)刺激的RAW264.7小鼠巨噬细胞中,反式-对甲氧基肉桂酸乙酯((E)-Ethyl p-methoxycinnamate)(10-50 μM)具有剂量依赖性抗炎活性。25.6 μM(IC50)时,抑制一氧化氮(NO)生成50%;50 μM时,NO抑制率达78%,采用Griess试剂法检测[1]
它还浓度依赖性抑制前列腺素E2(PGE2)合成:32.1 μM(IC50)时PGE2生成减少50%,50 μM时抑制率达72%,通过夹心ELISA法检测[1] qPCR分析显示,50 μM该化合物下调iNOS mRNA表达68%、COX-2 mRNA表达63%;蛋白质印迹法证实蛋白水平降低:50 μM时iNOS减少71%、COX-2减少65%[1] 此外,它抑制促炎细胞因子分泌:50 μM时肿瘤坏死因子-α(TNF-α)减少67%,白细胞介素-6(IL-6)减少61%。浓度高达100 μM时,对RAW264.7细胞无显著细胞毒性(MTT法:存活率>92%)[1] |
| 体内研究 (In Vivo) |
在佛波酯(TPA,12-O-十四酰佛波醇-13-乙酸酯)诱导的ICR小鼠(20-25 g)耳肿胀模型中,于TPA刺激前30分钟局部涂抹反式-对甲氧基肉桂酸乙酯((E)-Ethyl p-methoxycinnamate)(20 mg/kg或40 mg/kg),呈剂量依赖性抑制肿胀形成。20 mg/kg剂量组耳肿胀抑制率42%,40 mg/kg剂量组达65%,相较于溶媒对照组[1]
耳组织病理学检查显示,40 mg/kg剂量组炎症细胞浸润减少70%,血管扩张和水肿减轻,真皮厚度减少58%(H&E染色)[1] |
| 细胞实验 |
RAW264.7巨噬细胞抗炎实验:RAW264.7细胞在添加胎牛血清的DMEM中培养,以5×10⁴个/孔接种到96孔板(用于NO/PGE2检测)或2×10⁵个/孔接种到6孔板(用于蛋白/mRNA分析),贴壁培养24小时[1]
细胞用反式-对甲氧基肉桂酸乙酯((E)-Ethyl p-methoxycinnamate)(10-50 μM)预处理1小时后,加入LPS(1 μg/mL)刺激24小时。收集上清液,采用Griess试剂法定量NO,ELISA法检测PGE2[1] 蛋白提取:用RIPA缓冲液裂解细胞,通过蛋白质印迹法(SDS-PAGE电泳、转膜、抗体孵育、ECL显色)检测iNOS/COX-2蛋白水平;mRNA分析:Trizol法提取总RNA,逆转录为cDNA后,qPCR定量iNOS/COX-2 mRNA表达(β-肌动蛋白作为内参)[1] |
| 动物实验 |
TPA-induced mouse ear edema model: Male ICR mice (20-25 g, n=6 per group) were randomly divided into control, model, 20 mg/kg, and 40 mg/kg treatment groups. (E)-Ethyl p-methoxycinnamate was dissolved in 5% DMSO + 95% ethanol to prepare 20 mg/mL and 40 mg/mL solutions, and 10 μL/ear was topically applied to the left ear of mice [1]
Thirty minutes later, the left ear of model and treatment groups was treated with TPA (2.5 μg/ear, dissolved in 20 μL acetone), while the right ear served as a control. Twenty-four hours after TPA challenge, ear thickness was measured with a vernier caliper, and edema rate was calculated as [(left ear thickness - right ear thickness)/right ear thickness × 100%] [1] Mice were euthanized, and left ear tissues were fixed in 4% paraformaldehyde, embedded in paraffin, sectioned, and stained with H&E for histological observation of inflammatory cell infiltration and tissue morphology [1] |
| 毒性/毒理 (Toxicokinetics/TK) |
In vitro toxicity: Ethyl (E)-p-methoxycinnamate at concentrations up to 100 μM did not show significant cytotoxicity to RAW264.7 cells (MTT assay: cell viability >92% vs. control group) [1] In vivo toxicity: Topical application of 40 mg/kg ethyl (E)-p-methoxycinnamate in ICR mice did not cause abnormal behavior, significant weight changes, or histopathological abnormalities of the liver, kidneys, or heart within 24 hours [1]
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| 参考文献 | |
| 其他信息 |
4-Methoxycinnamate ethyl ester is a cinnamic ester. It has been reported that 4-methoxycinnamate ethyl ester exists in galangal and ginger flowers, and relevant data are available.
(E)-ethyl p-methoxycinnamate is a natural phenylpropanoid compound, which was isolated from the dried rhizome of Kaempferia galangal L. [1] The extraction method is to extract the crushed Kaempferia galangal rhizome by refluxing with 95% ethanol, concentrate the extract, and then purify it by silica gel column chromatography (petroleum ether-ethyl acetate gradient elution) and gel column chromatography [1] Its chemical structure was identified by spectroscopic analysis (UV, IR, ¹H-NMR, ¹³C-NMR, MS), and it was confirmed to be the trans isomer of ethyl p-methoxycinnamate [1] Its anti-inflammatory mechanism involves downregulating the mRNA and protein expression of iNOS and COX-2, thereby reducing the production of inflammatory mediators (NO, PGE2) and pro-inflammatory cytokines (TNF-α, IL-6) [1]. |
| 分子式 |
C12H14O3
|
|---|---|
| 分子量 |
206.2378
|
| 精确质量 |
206.094
|
| CAS号 |
24393-56-4
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| PubChem CID |
5281783
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| 外观&性状 |
Light yellow to yellow solid powder
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| 密度 |
1.1±0.1 g/cm3
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| 沸点 |
325.1±17.0 °C at 760 mmHg
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| 熔点 |
49ºC
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| 闪点 |
133.8±15.5 °C
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| 蒸汽压 |
0.0±0.7 mmHg at 25°C
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| 折射率 |
1.540
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| LogP |
2.65
|
| tPSA |
35.53
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| 氢键供体(HBD)数目 |
0
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| 氢键受体(HBA)数目 |
3
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| 可旋转键数目(RBC) |
5
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| 重原子数目 |
15
|
| 分子复杂度/Complexity |
215
|
| 定义原子立体中心数目 |
0
|
| SMILES |
CCOC(=O)/C=C/C1=CC=C(C=C1)OC
|
| InChi Key |
DHNGCHLFKUPGPX-RMKNXTFCSA-N
|
| InChi Code |
InChI=1S/C12H14O3/c1-3-15-12(13)9-6-10-4-7-11(14-2)8-5-10/h4-9H,3H2,1-2H3/b9-6+
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| 化学名 |
ethyl (E)-3-(4-methoxyphenyl)prop-2-enoate
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外实验) |
DMSO : ~100 mg/mL (~484.87 mM)
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|---|---|
| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (12.12 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: 2.5 mg/mL (12.12 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 悬浊液; 超声助溶。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (12.12 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8487 mL | 24.2436 mL | 48.4872 mL | |
| 5 mM | 0.9697 mL | 4.8487 mL | 9.6974 mL | |
| 10 mM | 0.4849 mL | 2.4244 mL | 4.8487 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。