PF-3845
作者：齐岳
发布时间：2023-09-11
09:05:16
点击数：
产品名称：PF-3845
产品描述：
| 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 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 45.7 mg/mL (100 mM)
Ethanol: 22.8 mg/mL (50 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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