aladdin 阿拉丁 A413448 AZ876 898800-26-5 99%

中文名：AZ876

英文名：AZ876

纯度：Moligand™，≥99%

货号：A413448

Cas号：898800-26-5

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

AZ876 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.

Targets

LXRα ; LXRβ 0.007 μM(Ki); 0.011 μM(Ki)

In vitro

In 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 vivo

AZ876 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.

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