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Datasheet of LXR623
Description: WAY-252623 (LXR-623) is a highly selective and orally bioavailable synthetic modulator of 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 .
Chemical Information Catalog
DC2072
Purity of current batch:
>98%
Molecular Weight (MW)
422.778
Molecular Formula
C21H12ClF5N2
CAS No.
875787-07-8
Solubility (25째C)
DMSO
Storage
Store at -20째C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20째C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.