貨號	規(guī)格	價格	上海	北京	武漢	南京
S81052-5mg	99.6%	￥272.00 S81052-5mg ￥272.00 現(xiàn)貨	9 9	-	-	-
S81052-10mg	≥98%	￥408.00 S81052-10mg ￥408.00 2-3天	0 貨期：2-3天	-	-	-
S81052-50mg	≥98%	￥1428.00 S81052-50mg ￥1428.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.

產(chǎn)品描述：

LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.

靶點：

IC50: 24 nM (LXR-α), 179 nM (LXR-β);LiverXReceptor

體內(nèi)研究：

LXR-623 (400 mg/kg, p.o.) crosses the blood-brain barrier, induces target gene expression, and achieves therapeutic levels in GBM cells in the brain with minimal activity in the periphery. LXR-623 inhibits tumor growth, promotes tumor cell death, and prolongs the survival of mice bearing intracranial patient-derived GBMs. LXR-623 (1.5, 5 mg/kg/day) significantly reduces progression of atherosclerosis in animals compared with the placebo group. WAY-252623 (15 and 50 mg/kg) results in a significant reduction of atherosclerosis in a dose-dependent manner. WAY-252623 (20, 60, and 120 mg/kg/day, p.o.) displays neutral lipid effects in this CETP-expressing Syrian hamster. Moreover, LXR-623 (50 mg/kg) induces gene expression in rodent peripheral blood cells in rat. LXR-623 (0, 15 and 50 mg/kg) dose-dependently upregulates transcription of ABCA1 and ABCG1 in monkey whole blood cells proportional to dose

參考文獻(xiàn)：

1. Villa GR, et al. An LXR-Cholesterol Axis Creates a Metabolic Co-Dependency for Brain Cancers. Cancer Cell. 2016 Nov 14;30(5):683-693. 2. Giannarelli C, et al. Synergistic effect of liver X receptor activation and simvastatin on plaque regression and stabilization: an magnetic resonance imaging study in a model of advanced atherosclerosis. Eur Heart J. 2012 Jan;33(2):264-73. 3. Quinet EM, et al. LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse. J Lipid Res. 2009 Dec;50(12):2358-70. 4. DiBlasio-Smith EA, et al. Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells. J Transl Med. 2008 Oct 16;6:59.

溶解性：

DMSO : ≥ 47 mg/mL (111.17 mM)

保存條件：

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.365 ml	11.827 ml	23.653 ml
5 mM	0.473 ml	2.365 ml	4.731 ml
10 mM	0.237 ml	1.183 ml	2.365 ml
50 mM	0.047 ml	0.237 ml	0.473 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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LXR-623 ( WAY 252623)

2H-Indazole, 2-[(2-chloro-4-fluorophenyl)Methyl]-3-(4-fluorophenyl)-7-(trifluoroMethyl)-