PF-3845
作者：齊岳
發(fā)布時(shí)間：2023-09-11
09:05:16
點(diǎn)擊數(shù)：
產(chǎn)品名稱：PF-3845
產(chǎn)品描述：
| 產(chǎn)品描述 | PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2. |
| 靶點(diǎn)活性 | FAAH:230 nM(Ki) |
| 體外活性 | PF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile. [1] |
| 體內(nèi)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 |
存儲(chǔ)
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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