Brief Description

WAY-252623 (LXR-623) is a highly selective and orally bioavailable synthetic modulator of LXR.
Target: LXR
in vitro: In nonhuman primates with normal lipid levels, WAY-252623 significantly reduced total (50-55%) and LDL-cholesterol (LDLc) (70-77%) in a time- and dose-dependent manner as well as increased expression of the target genes ABCA1/G1 in peripheral blood cells.
in vivo: LXR-623 was absorbed rapidly with peak concentrations (C(max)) achieved at approximately 2 hours. The C(max) and area under the concentration-time curve increased in a dose-proportional manner. The mean terminal disposition half-life was between 41 and 43 hours independently of dose. LXR activation resulted in a dose-dependent increase in ABCA1 and ABCG1 expression. Twelve cynomolgous monkeys maintained on normal chow were orally dosed with 0, 15 and 50 mg/kg/day of LXR-623 (n = 4 per dose group). Blood was collected prior to the first dose (day 0) to serve as a baseline and again on day 7. RNA prepared from whole blood was used for gene expression analysis of ABCA1 and ABCG1 by qPCR. In contrast to rodents, ABCG1 changed with much greater magnitude in primate blood cells than ABCA1 in response to LXR-623 at all doses tested.

Solubility

DMSO 47 mg/ml

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Storage conditions

Store at -20°C 2 years

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