Table 2.

Exposure correlations in vitro/in vivo

Species, strain	In vitro IC50, nm	Turnover half-life, min	In vivo IC20, nm	In vivo IC50, nm
Mouse, C57BL/6	2.7 ± 0.82	47 (37–64)	1.8 (1.5–2.1)	4.7
Guinea pig, DH	2.0 ± 1.3	53 (34–121)	0.5 (0.3–0.7)	1.8
Mouse, Tg2576	38 ± 11	NA	NA	NA

In vitro IC₅₀ in primary neurons incubated with AZ-4217 (±SD). Turnover half-life of Aβ40 in brain (k_out, estimate and 95% planar confidence interval). No turnover half-life could be determined in Tg2576 due to a single time point effect readout. In vivo IC₂₀ is expressed as free AZ-4217 concentration in brain (estimate and 95% planar confidence interval). Calculated in vivo IC₅₀ for Aβ40 in brain as free AZ-4217 concentration in brain.