Redafamdastat

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Redafamdastat

CAS No. : 1020315-31-4

MCE 国际站：Redafamdastat

产品活性：Redafamdastat (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。是是

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

作用靶点：FAAH  |  Autophagy

In Vitro: Redafamdastat 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). Redafamdastat has exquisite selectivity for FAAH relative to other members of the serine hydrolase superfamily as demonstrated by competitive activity-based protein profiling. Redafamdastat completely inhibits FAAH in human and mouse membrane proteomes at both 10 and 100 μM with no off targets. Redafamdastat is completely selective for FAAH, and none of the other FP-reactive serine hydrolases in the tested tissues are inhibited by Redafamdastat even at 100 μM.

In Vivo: Oral administration of Redafamdastat 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 Redafamdastat 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.), Redafamdastat 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 Redafamdastat at 1 and 10 mg/kg p.o. by competitive activity-based protein profiling (ABPP) study.

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