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PF-04457845

CAS No. : 1020315-31-4

MCE 站：PF-04457845

产品活性：PF-04457845 是一种高效选择性的 FAAH 抑制剂，作用于 hFAAH 和 rFAAH，IC₅₀ 分别为 7.2±0.63 nM 和 7.4±0.62 nM。

研究领域：Metabolic Enzyme/Protease  |  Neuronal Signaling  |  Autophagy

作用靶点：FAAH  |  Autophagy

In Vitro: PF-04457845 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH with high in vitro potency (k_inact/K_i and IC₅₀ values of 40300 M^-1s^-1 and 7.2 nM, respectively, for human FAAH). PF-04457845 has exquisite selectivity for FAAH relative to other members of the serine hydrolase superfamily as demonstrated by competitive activity-based protein profiling. PF-04457845 completely inhibits FAAH in human and mouse membrane proteomes at both 10 and 100 μM with no off targets. PF-04457845 is completely selective for FAAH, and none of the other FP-reactive serine hydrolases in the tested tissues are inhibited by PF-04457845 even at 100 μM.

In Vivo: Oral administration of PF-04457845 at 0.1 mg/kg results in efficacy comparable to that of naproxen at 10 mg/kg in a rat model of inflammatory pain. Oral administration of PF-04457845 causes a significant inhibition of mechanical allodynia measured after 4 h with a minimum effective dose (MED) of 0.1 mg/kg. Furthermore, at 0.1 mg/kg (p.o.), PF-04457845 inhibits the pain response to a comparable degree as the nonsteroidal anti-inflammatory drug naproxen at 10 mg/kg. FAAH is confirmed to be completely inhibited in mice treated with PF-04457845 at 1 and 10 mg/kg p.o. by competitive activity-based protein profiling (ABPP) study.

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