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.
MedKoo Cat#: 555189
Name: PF-06795071
CAS#: 2075629-81-9
Chemical Formula: C18H17F4N3O3
Exact Mass: 399.1206
Molecular Weight: 399.35
Elemental Analysis: C, 54.14; H, 4.29; F, 19.03; N, 10.52; O, 12.02
The following data is based on the product molecular weight 399.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
