鸡豆黄素A ≥98%(HPLC),分析标准品
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| 包装规格: | 20mg in glass bottle |
| 溶解性: | DMSO : ≥ 50 mg/mL (175.90 mM) |
| 储备液保存: | -80°C, 2 years -20°C, 1 year |
| 体内实验: | 1、请依序添加每种溶剂: 10% DMSO→40% PEG300→5% Tween-80→45% Saline Solubility: ≥ 2.5 mg/mL (8.79 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL。 2、请依序添加每种溶剂: 10% DMSO→90% Corn Oil Solubility: ≥ 2.5 mg/mL (8.79 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
| 靶点: | IC50: 1.8 μM (mouse FAAH), 1.4 μM (rat FAAH), 2.4 μM (human FAAH) |
| 体外研究: | 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)。 |
| 体内研究: | 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。 |
| 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 <10% of added substrate is metabolized. For the human FAAH samples, <5% of the [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). |
| 保存条件: | 2-8℃ |
| 注意事项: | 1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。 |
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