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产品价格:电议      采购度:1632      原产地:美洲
发布时间:2021/6/30 9:57:48 所属地区:国外 国外
简要描述:
XL041 (BMS-852927) 是一种 LXRβ 选择性激动剂。
标签:BMS-852927
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CAS No. : 1256918-39-4
MCE 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
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.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Clinical Compound Library | Anti-Cardiovascular Disease Compound Library | T0901317 | GSK2033 | LXR-623 | 27-Hydroxycholesterol | (20S)-Protopanaxatriol | SR9243 | SR9238 | 24-Hydroxycholesterol | AZ876 | Saikosaponin A | Yamogenin | Nagilactone B | DMHCA | Gymnestrogenin | Iristectorigenin B | LXRβ agonist-2
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更新时间:2024/1/2 10:12:11
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