Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LXR-623 (WAY 252623) 是一种LXRα部分激动剂和LXRβ完全激动剂,可透过血脑屏障,IC50分别为 179 nM 和 24 nM 。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 196 | 现货 | ||
5 mg | ¥ 453 | 现货 | ||
10 mg | ¥ 645 | 现货 | ||
25 mg | ¥ 1,320 | 现货 | ||
50 mg | ¥ 2,570 | 现货 | ||
100 mg | ¥ 3,880 | 现货 | ||
200 mg | ¥ 5,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 525 | 现货 |
产品描述 | LXR-623 (WAY 252623) is an orally bioavailable and highly specifical synthetic modulator of LXR. |
靶点活性 | LXRβ:24 nM, LXRα:179 nM |
体外活性 | LXR-623 suppresses LDLR expression, increases expression of the ABCA1 efflux transporter, and induces substantial cell death in all of the GBM samples tested. The brain metastatic breast cancer cell line MDA-MB-361, which harbors ERBB2 amplification, is also highly sensitive to LXR-623- dependent cell death in a concentration-dependent manner. LXR-623 inhibits LDL uptake and induces cholesterol efflux in GBM cells, resulting in a significant reduction in cellular cholesterol content. Normal brain cell insensitivity to LXR-623 may be due to reliance on endogenous synthesis of cholesterol and intact negative feedback through synthesis of endogenous oxysterols[3]. |
体内活性 | LXR-623 is absorbed rapidly with peak concentrations (Cmax) achieved at approximately 2 hours. The Cmax and area under the concentration-time curve increases in a dose-proportional manner. The mean terminal disposition half-life is between 41 and 43 hours independently of dose. In a low-density lipoprotein (LDL) receptor, (LDLr) knockout mouse model of atherosclerosis, LXR-623 administered orally upregulates intestinal ABCG5 and ABCG8 and reduces atheroma burden without altering serum or hepatic cholesterol and trig-lycerides. LXR-623 shows brain penetration and causes tumor regression in a GBM(glioblastomas) mouse model, reducing cholesterol and inducing cell death[1]. |
细胞实验 | The purified PBMC are resuspended in culture medium (RPMI + 10% fetal calf serum + 1% penicillin/streptomycin with 1% L-glutamine), transferred to 6-well (9.5 cm2 each) tissue culture dishes at approximately 5 × 106 cells per well, and 2 μM LXR-623 or vehicle (DMSO) are added. After 18 hours of culture, RNA isolation and qPCR analysis for LXRα, LXRβ, ABCA1, ABCG1, and PLTP is performed.(Only for Reference) |
别名 | LXR623, WAY 252623 |
分子量 | 422.78 |
分子式 | C21H12ClF5N2 |
CAS No. | 875787-07-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 42.3 mg/mL (100 mM)
Ethanol: 42.3 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.3653 mL | 11.8265 mL | 23.653 mL | 59.1324 mL |
5 mM | 0.4731 mL | 2.3653 mL | 4.7306 mL | 11.8265 mL | |
10 mM | 0.2365 mL | 1.1826 mL | 2.3653 mL | 5.9132 mL | |
20 mM | 0.1183 mL | 0.5913 mL | 1.1826 mL | 2.9566 mL | |
50 mM | 0.0473 mL | 0.2365 mL | 0.4731 mL | 1.1826 mL | |
100 mM | 0.0237 mL | 0.1183 mL | 0.2365 mL | 0.5913 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LXR-623 875787-07-8 Metabolism Liver X Receptor Inhibitor Liver X receptor WAY-252623 LXR LXR623 inhibit WAY 252623 LXR 623 WAY252623 inhibitor