LXR-623 (Synonyms: WAY-252623) |
カタログ番号GC13954 |
LXR-623 は、脳浸透性部分 LXRα および完全 LXRβ アゴニストであり、IC50 はそれぞれ 24 nM および 179 nM です。
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Cas No.: 875787-07-8
Sample solution is provided at 25 µL, 10mM.
LXR-623 is an agonist of liver X-receptor with IC50 values of 179nM and 24nM for LXR-α and LXR-β, respectively [1].
LXR-623 is a partial agonist of LXR which regulates the transcription of genes involved in cellular cholesterol homeostasis. As the LXR agonist, LXR-623 is used to enhance reverse cholesterol transport through up-regulating cholesterol transporters. To rodents, orally dosed LXR-623 increases the transcription level of ABCA1 and ABCG1 in peripheral blood cells. To human, LXR-623 also significantly increases ABCA1 and ABCG1 both in PBMC cells and in T- and B-cells. In addition, in mouse model of atherosclerosis, LXR-623 is found to up-regulate intestinal ABCG5 and ABCG8. In cynomolgus monkeys, LXR-623 up-regulates ABCA1 and ABCG1 in whole blood. Besides that, LXR-623 is proposed to be used in treatment of Alzheimer’s disease since it can lower the level of amyloid-βin brain [1, 2].
References:
[1] Katz A, Udata C, Ott E, et al. Safety, Pharmacokinetics, and Pharmacodynamics of Single Doses of LXR‐623, a Novel Liver X‐Receptor Agonist, in Healthy Participants. The Journal of Clinical Pharmacology, 2009, 49(6): 643-649.
[2] DiBlasio-Smith E A, Arai M, Quinet E M, et al. Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells. J Transl Med, 2008, 6: 59.
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