Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF3845 是一种有效的、选择性的和不可逆的脂肪酸酰胺水解酶(FAAH)抑制剂,Ki 为 230 nM。它是将 FAAH 的丝氨酸亲核试剂氨基甲酸酯化的共价抑制剂,可以减少疼痛感、炎症和焦虑或抑郁。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 268 | 现货 | ||
5 mg | ¥ 423 | 现货 | ||
10 mg | ¥ 772 | 现货 | ||
25 mg | ¥ 1,580 | 现货 | ||
50 mg | ¥ 2,970 | 现货 | ||
100 mg | ¥ 4,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 425 | 现货 |
产品描述 | PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2. |
靶点活性 | FAAH:230 nM(Ki) |
体外活性 | PF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile. [1] |
体内活性 | PF-3845 treated mice (10 mg/kg, i.p.) shows rapid and complete inactivation of FAAH in the brain, as judged by competitive activity-based protein profiling (ABPP) with the serine hydrolase-directed probe fluorophosphonate (FP)-rhodamine. PF-3845 shows a long duration of action up to 24 hour. PF-3845-treated mice also shows dramatic (>10-fold) elevation in brain levels of AEA and other NAEs (N-pamitoyl ethanolamine [PEA] and N-oleoyl ethanolamine [OEA]). FAAH is AEA-degrading enzyme fatty acid amide hydrolase. PF-3845 (1–30 mg/kg, oral administration [p.o.]) causes a dose dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg (rats are analyzed at 4 hour post dosing with PF-3845). At higher doses (10 and 30 mg/kg), PF-3845 inhibits pain responses to an equivalent, if not greater, degree than the nonsteroidal anti-inflammatory drug naproxen (10 mg/kg, p.o.). [1] PF-3845 (10 mg/kg, i.p.) significantly reverses LPS-induced tactile allodynia, but doesn't modify paw withdrawal thresholds in the saline-injected paw. [2] |
分子量 | 456.46 |
分子式 | C24H23F3N4O2 |
CAS No. | 1196109-52-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (219 mM)
Ethanol: 22.8 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.1908 mL | 10.9539 mL | 21.9077 mL | 54.7693 mL |
5 mM | 0.4382 mL | 2.1908 mL | 4.3815 mL | 10.9539 mL | |
10 mM | 0.2191 mL | 1.0954 mL | 2.1908 mL | 5.4769 mL | |
20 mM | 0.1095 mL | 0.5477 mL | 1.0954 mL | 2.7385 mL | |
50 mM | 0.0438 mL | 0.2191 mL | 0.4382 mL | 1.0954 mL | |
DMSO | 100 mM | 0.0219 mL | 0.1095 mL | 0.2191 mL | 0.5477 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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