PF-06751979 is a potent, and brain penetrant β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor which lacks hypopigmentation. PF-06751979 showed BACE1 IC50 = 7.3 nM, and BACE2 IC50= 273 nM. PF-06751979 displays excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases, including BACE2. Chronic dosing of 64 for up to 9 months in dog model did not reveal any observation of hair coat color (pigmentation) changes and suggests a key differentiator over current BACE1 inhibitors that are nonselective against BACE2 in later stage clinical development.
MedKoo Cat#: 555239
Name: PF-06751979 free base
CAS#: 1818339-66-0 (free base)
Chemical Formula: C18H19F2N5O3S2
Exact Mass: 455.0897
Molecular Weight: 455.50
Elemental Analysis: C, 47.46; H, 4.20; F, 8.34; N, 15.38; O, 10.54; S, 14.08
The following data is based on the product molecular weight 455.50 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 |
