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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
BMS-852927
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥4425.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1100.0 |
| 规格： | 5 mg | 产品价格： | ￥3300.0 |
| 规格： | 10 mg | 产品价格： | ￥5000.0 |
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XL041
CAS No. : 1256918-39-4
MCE 国际站：XL041
产品活性：XL041 (BMS-852927) 是一种 LXRβ 选择性激动剂。
研究领域：Metabolic Enzyme/Protease | Vitamin D Related/Nuclear Receptor
作用靶点：LXR
In Vitro: XL041 (BMS-852927) is an LXRβ-selective agonist with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays. XL041 is potent, with an EC50=9 nM and 26% activity in an in vitro human whole-blood endogenous target gene activation assay (WBA). BMS-852927 has similar binding affinity to LXRα and LXRβ (19 and 12 nM, respectively).
In Vivo: XL041 (BMS-852927), has a very favorable profile at efficacious doses in cynomolgus monkeys and 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. In a separate study, XL041 inhibits the progression of atherosclerosis in a 12 week study in LDLR 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.
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