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. Author manuscript; available in PMC: 2013 Jul 1.
Published in final edited form as: Bioorg Med Chem Lett. 2012 May 8;22(13):4413–4417. doi: 10.1016/j.bmcl.2012.04.126

Table 6.

In vivo properties of selected Rev-erbα agonists

Compound a[Plasma] (μM) [Brain] (μM) eb.p. (%)
b 1 0.25 0.35 140
b 12h 0.53 0.24 53
b 12j 0.54 1.3 242
b 12e 0.53 0.53 100
c 12e 6.7 d8.7 100
a

Mice sacrificed at t = 2h. Brain and plasma levels of drug determined;

b

Mice dosed 10 mg/kg IP in 10:10:80 DMSO:Tween:water;

c

Mice dosed 50 mg/kg IP in 15% cremaphor EL;

d

brain levels at 8h;

e

b.p. = brain penetration.