L 888607 is a potent, and selective CRTH2 (also known as DP2) agonist with a Ki of 0.8±0.4 nM.
L 888607 (L-888,607) is administered to mice either intravenously (i.v.) or orally (p.o.) to determine its pharmacokinetic profile over an 8-h period. After an intravenous administration of 5 mg/kg L 888607, blood analysis reveals a peak level (Cmax) of 36.1 μM, a half-life (t1/2) of 2.9 h, a trough level at 8 h (C8h) of 3.5 μM, and an area under the curve0-8h of 87.1 μM. After oral administration of 20 mg/kg L 888607, blood analysis reveals a Cmax of 31.6 μM, a t1/2 of 4 h, a C8h at 8 h of 15.4 μM, an area under the curve0-8h of 166 μM, and a bioavailability of 48%[1].
[1]. Gervais FG, Identification of a potent and selective synthetic agonist at the CRTH2 receptor. Mol Pharmacol. 2005 Jun;67(6):1834-9. [2]. Ulven T, et al. Novel CRTH2 antagonists: a review of patents from 2006 to 2009. Expert Opin Ther Pat. 2010 Nov;20(11):1505-30.