Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XL041 (BMS-852927) is an agonist of LXRβ-selective.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | 待询 | 8-10周 | ||
25 mg | 待询 | 8-10周 | ||
50 mg | 待询 | 8-10周 | ||
100 mg | 待询 | 8-10周 | ||
1 mL * 10 mM (in DMSO) | 待询 | 8-10周 |
产品描述 | XL041 (BMS-852927) is an agonist of LXRβ-selective. |
体外活性 | XL041 (BMS-852927) is an LXRβ-selective agonist with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays. BMS-852927 has similar binding affinity to LXRα and LXRβ (19 and 12 nM, respectively)[1]. XL041 is potent, with an EC50=9 nM and 26% activity in an in vitro human whole-blood endogenous target gene activation assay (WBA). |
体内活性 | XL041 (BMS-852927) which has a very favorable profile at efficacious doses in cynomolgus monkeys and mice. In a separate study, XL041 inhibits the progression of atherosclerosis in a 12 week study in LDLR KO mice. XL041 pre-treatment of C57BL/6J mice for 7 days results in potent, dose-dependent stimulation of cholesterol efflux in this system; reaching a maximum in the 3 mg/kg/day dose group of 70% above vehicle in the initial efflux rate. Similar results are obtained in LDLR knockout (KO) mice. Importantly, the dose response for inhibition of atherosclerosis (0.1-3 mg/kg/day) is similar to the dose response for macrophage reverse cholesterol transport (RCT) stimulation (0.03-3 mg/kg/day), a major underlying mechanism through which LXR agonists affect the disease[1]. |
别名 | BMS-852927 |
分子量 | 609.51 |
分子式 | C29H28Cl2F2N2O4S |
CAS No. | 1256918-39-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (164.07 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.6407 mL | 8.2033 mL | 16.4066 mL | 41.0166 mL |
5 mM | 0.3281 mL | 1.6407 mL | 3.2813 mL | 8.2033 mL | |
10 mM | 0.1641 mL | 0.8203 mL | 1.6407 mL | 4.1017 mL | |
20 mM | 0.082 mL | 0.4102 mL | 0.8203 mL | 2.0508 mL | |
50 mM | 0.0328 mL | 0.1641 mL | 0.3281 mL | 0.8203 mL | |
100 mM | 0.0164 mL | 0.082 mL | 0.1641 mL | 0.4102 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。
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