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note
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3, 400 MHz) δ 7.80 (m, 4H), 7.08 (m, 1H), 6.42 (m, 1H), 5.16 (d, 1H), 4.22 (d, 1H), 3.71 (s, 3H), 3.02 (d, 1H), 2.60 (d, 1H), 2.45 (m, 1H), 1.97 (m, 2H), 1.75 (m, 1H), 1.58 (m, 1H), 1.07 (m, 1H).
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14
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0035942322
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Efficacy of γ-secretase inhibitors in intact cells was measured using HEK293 cells expressing human APP with both Swedish and London mutations. The cells were grown in 96-well plate with 100 μL media per well, and were changed to fresh media and incubated with γ-secretase inhibitor for 4 h. Ten microliters of conditioned media was used to measure Aβ40 using ECL technology as described in the following reference. L. Zhang, L. Song, G. Terracina, Y. Liu, B. Pramanik, and E. Parker Biochemistry 40 2001 5049
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15
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77954212903
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note
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For example, Compound 17b showed 86% inhibition of Aβ40 in plasma and 48% in brain at 10 mg/kg po and compound 15c showed 101% inhibition of Aβ40 in plasma and 71% in brain at 10 mg/kg po.
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16
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0035100437
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Following the oral dosing at 10 mpk in 20% HPBCD, AUC in rats was measured over a period of 6 h, using cassette-accelerated rapid rat screen (CARRS): W.A. Korfmacher, K.A. Cox, K.J. Ng, J. Veals, Y. Hsieh, S. Wainhaus, L. Broske, D. Prelusky, A. Nomeir, and R.E. White Rapid Commun. Mass Spectrom. 15 2001 335
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Prelusky, D.8
Nomeir, A.9
White, R.E.10
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