| CAS |
No.491-80-5 |
| 中文名称 |
鹰嘴豆芽素A(10mM in DMSO,无菌） |
| 英文名称 |
Biochanin A(10mM in DMSO，Sterile） |
| 分子式 |
C16H12O5 |
| 分子量 |
284.27 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
FAAH |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
Biochanin A 是一种脂肪酸酰胺水解酶 (FAAH) 抑制剂。 |
| 生物活性 |
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor， which inhibits FAAH with IC50s of 1.8， 1.4 and 2.4 μM for mouse， rat， and human FAAH， respectively.[1] |
| IC50 |
IC50: 1.8 μM (mouse FAAH)， 1.4 μM (rat FAAH)， 2.4 μM (human FAAH)[1] |
| In Vitro |
Biochanin A 抑制小鼠、大鼠和人 FAAH 对 0.5 μM AEA 的水解，IC50 分别为 1.8、1.4 和 2.4 μM。FAAH 被 Biochanin A 抑制，pIC50 值为 6.21±0.02，对应的 IC50 值为 0.62 μM。Biochanin A 在高纳摩尔-低微摩尔浓度下显著抑制 URB597 敏感的氚滞留。实验使用人 FAAH 和 0.5 μM [3H]AEA 进行，测定条件可提供更高的利用率，该活性在低微摩尔范围内仍被 Biochanin A、Genistein、Formononetin 和 Daidzein 抑制 (IC50 分别为 6.0、8.4、12 和 30 μM)[1]。 |
| In Vivo |
Biochanin A 的测试剂量为 30、100 和 300 μg。最高剂量还以一种被 AM251 拮抗的方式降低了福尔马林诱导的 ERK 磷酸化。因此，Biochanin A 在爪子局部给药后表现得像 URB597。在麻醉小鼠中，URB597 (30 μg i.pl.) 和 Biochanin A (100 μg i.pl.) 均抑制足底注射福尔马林产生的细胞外信号调节激酶的脊髓磷酸化。CB1 受体拮抗剂/反向激动剂 AM251 (30 μg i.pl.) 可显著降低这两种化合物的作用。Biochanin A (15 mg/k iv) 不会增加大脑 AEA 浓度，但会适度增强 10 mg/kg iv AEA 在四分体测试中的作用。Biochanin A (15 mg/kg iv) 本身没有影响，但会显著增强 AEA (10 mg/kg iv) 的作用[1]。 |
| 动物实验 |
Mice[1] ICR mice are used for the behavioural tests measuring spontaneous activity (over a 10 min testing period)， rectal temperature， ring immobility (over a 5 min testing period) and nociceptive threshold (tail flick tests). AEA and Biochanin A are dissolved in a vehicle consisting of ethanol， Emulphor-620 and physiological saline in a ratio of 1:1:18 v/v， and administered i.v. to the animals via the tail vein (injection volume 10 μL/g body weight). The degree of antinociception is expressed as percentage of maximum possible effect (%MPE)， defined as [(test-control time)/(10-control time)]×100. |
| 激酶实验 |
For experiments with FAAH， rat liver homogenates， mouse brain homogenates and membranes from COS7 cells transfected with the human enzyme are used. Frozen (?80°C) livers from adult C57BL/6 mice and frozen brains (minus cerebella) from adult Wistar or Sprague-Dawley rats are thawed and homogenized in 20 mM HEPES， 1 mM MgCl2， pH 7. The homogenates are centrifuged at ~35000×g for 20 min at 4°C. After resuspension in buffer followed by recentrifugation and a second resuspension in buffer， the pellets are incubated at 37°C for 15 min. This incubation is undertaken in order to hydrolyse all endogenous FAAH substrates. The homogenates are then centrifuged as above， recentrifuged and resuspended in 50 mM Tris-HCl buffer， pH 7.4， containing 1 mM EDTA and 3 mM MgCl2. The homogenates are then frozen at ?80°C in aliquots until used for assay. FAAH is assayed in the homogenates and in the COS7 cell membranes using 0.5 μM (unless otherwise stated) [3H]AEA labelled in the ethanolamine part of the molecule. Blank values are obtained by the use of buffer rather than homogenate. In the experiments comparing effects of Biochanin A upon FAAH and FAAH-2， the same assay is used but with 16 nM [3H]oleoylethanolamide ([3H]OEA) as substrate and with an incubation phase at room temperature. The choice of OEA rather than AEA for FAAH-2 is motivated by the relative rates of hydrolysis: OEA is metabolized four times faster than AEA by FAAH-2， whereas for FAAH the rate of hydrolysis of OEA is about a third of that for AEA. When 0.5 μM [3H]AEA is used as substrate， assay conditions for rat brain and mouse liver are chosen so that 3H]AEA is metabolized in all cases. For 16 nM [3H]OEA， a limited supply of an expensive ligand meant that optimization is not possible， and the amount of substrate utilized is higher (34±1 and 0.5±0.1% for FAAH and its corresponding mock-transfected， respectively; 40±2 and 21±0.4 for FAAH-2 and its corresponding mock-transfected respectively)[1]. |
| 数据来源文献 |
[1]. Thors L， et al. Biochanin A， a naturally occurring inhibitor of fatty acid amide hydrolase. Br J Pharmacol. 2010 Jun;160(3):549-60. |
| 规格 |
1ml |
| 单位 |
瓶 |
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英语
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