2075629-81-9
中文名稱
PF-06795071
英文名稱
PF-06795071
CAS
2075629-81-9
分子式
C18H17F4N3O3
分子量
399.35
MOL 文件
2075629-81-9.mol
2075629-81-9 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點512.6±50.0 °C(Predicted)
密度1.58±0.1 g/cm3(Predicted)
酸度系數(shù)(pKa)13.42±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
應(yīng)用領(lǐng)域
用途一
PF-06795071 is a potent and selective covalent MAGL inhibitor with MAGL IC50 = 3 nM; FAAH IC50 = 3.1 μM; log D= 3.8; Cb,u/Cp,u = 1.4. PF-06795071 features a novel trifluoromethyl glycol leaving group which confers significant physicochemical property improvements as compared with earlier inhibitor series with more lipophilic leaving groups. The design strategy focused on identifying an optimized leaving group that delivers MAGL potency, serine hydrolase selectivity, and CNS exposure; while simultaneously, reducing LogD, improving solubility, and minimizing chemical lability. PF-06795071 achieves excellent CNS exposure, extended 2-AG elevation effect in vivo, and decreased brain inflammatory markers in response to an inflammatory challenge.