| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P408694-1ml |
1ml |
现货  |
|
| 英文别名 | 4-(3-(5-(trifluoromethyl)pyridin-2-yloxy)benzyl)-N-(pyridin-3-yl)piperidine-1-carboxamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | PF-3845 |
| 生化机理 | PF-3845 是一种强效、选择性和不可逆的 FAAH 抑制剂，Ki为 230 nM，对 FAAH2 的活性微乎其微。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 脂肪酸酰胺水解酶抑制剂 |
| 产品介绍 |
PF-3845是一种有效的，选择性的，不可逆的FAAH抑制剂，Ki为230 nM，对FAAH2几乎没有作用活性。A selective fatty acid amide hydrolase (FAAH) inhibitor. Information PF-3845 PF-3845 is a potent, selective and irreversible FAAH inhibitor with K i of 230 nM, showing negligible activity against FAAH2. PF-3845 selectively inhibits FAAH by carbamylating FAAH\'s serine nucleophile. In vivo 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 (10mg/kg, p.o.). 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. cell lines：NCI-H929, U266, RPMI-8226 and OPM2 MM cells Concentrations： Incubation Time： Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1CN(CCC1CC2=CC(=CC=C2)OC3=NC=C(C=C3)C(F)(F)F)C(=O)NC4=CN=CC=C4 |
| Reaxy-Rn | 20599234 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20599234&ln= |
| 象形图 | GHS06 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H301: 吞咽会中毒 |
| 预防措施声明 |
P301+P310: 如误吞咽：立即呼叫急救中心/医生。 |
| WGK Germany | 3 |
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