Home Metabolism Liver X Receptor agonist AZ876

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AZ876 Liver X Receptor agonist

Cat.No.S6427

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.
AZ876 Liver X Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 439.57

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Quality Control

Batch: S642701 DMSO]88 mg/mL]false]]]false]]]false Purity: 99.76%
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99.76

Solubility

In vitro
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DMSO : 88 mg/mL (200.19 mM)
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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 439.57 Formula

C24H29N3O3S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 898800-26-5 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C)(C)N1C(=O)C(=C(S1(=O)=O)C2=CC=CC=C2)NC3=CC=C(C=C3)N4CCCCC4

Mechanism of Action

Targets/IC50/Ki
LXRα
0.007 μM(Ki)
LXRβ
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, this compound is 196-fold and fivefold more potent than GW3965 on hLXRα and hLXRβ respectively. It is also more potent than GW3965 on mouse (m)LXRα (248-fold) and mLXRβ (10.5-fold). This chemical is four- to sevenfold more potent than GW3965 on the expression of ABCA1 mRNA in hamster and human blood PMN cells. It 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 this compound attenuates pathological cardiac hypertrophy in a murine model of chronic pressure overload without altering systemic blood pressure, implicating heart-specific effects. This compound treatment diminishes myocardial fibrosis and suppresses induction of profibrotic gene expression.
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