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AZ876

    
10mM in DMSO

AZ876

源叶(MedMol)
T99766 一键复制产品信息
898800-26-5
C24H29N3O3S
439.57
3(2H)​-​Isothiazolone,2-​(1,​1-​dimethylethyl)​-​5-​phenyl-​4-​[[4-​(1-​piperidinyl)​phenyl]​amino]​-​,1,​1-​dioxide
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
T99766-1ml
10mM in DMSO

¥720.00

6 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: 肝 X 受体激动剂;Liver X Receptor Agonists;;InformationAZ876 AZ876 is a novel high-affinity Liver X Receptor (LXR) agonist with Ki values of 0.007 μM and 0.011 μM for human LXRα and LXRβ respectively.TargetsLXRα ; LXRβ 0.007 μM(Ki); 0.011 μM(Ki)In vitroIn binding assays, AZ876 is 25-fold and 2.5-fold more potent than GW3965 on human (h)LXRα and hLXRβ respectively. In reporter transactivation assays, AZ876 is 196-fold and fivefold more potent than GW3965 on hLXRα and hLXRβ respectively. AZ876 is also more potent than GW3965 on mouse (m)LXRα (248-fold) and mLXRβ (10.5-fold). AZ876 is four- to sevenfold more potent than GW3965 on the expression of ABCA1 mRNA in hamster and human blood PMN cells. AZ876 is highly selective with respect to other nuclear hormone receptors, including retinoid X receptor, farnesoid X receptor, thyroid hormone receptor (TR)α or TRβ, when tested in agonist mode in fluorescence resonance energy transfer assays.In vivoAZ876 is a dual partial LXR agonist that has been shown to reduce atherosclerosis in mice without affecting liver or plasma triglyceride levels when administered in low dose. Chronic administration of the LXR agonist AZ876 attenuates pathological cardiac hypertrophy in a murine model of chronic pressure overload without altering systemic blood pressure, implicating heart-specific effects. AZ876 treatment diminishes myocardial fibrosis and suppresses induction of profibrotic gene expression.
体内研究: AZ876 (20 μmol/kg;口服;每日 1 次;3 周) 在 C57BL/6 小鼠的动脉粥样硬化模型中,显著降低病变面积,减少单核细胞黏附,增加心脏多不饱和脂肪酸水平,改善心脏功能。
保存条件: -80℃(运输条件:冰袋低温运输)
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.275 ml 11.375 ml 22.75 ml
5 mM 0.455 ml 2.275 ml 4.55 ml
10 mM 0.227 ml 1.137 ml 2.275 ml
50 mM 0.045 ml 0.227 ml 0.455 ml
注意: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

质检证书(COA)

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摩尔浓度计算器

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