AZ876

Catalog No.S6427

For research use only.

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 Chemical Structure

CAS No. 898800-26-5

Selleck's AZ876 has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description 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 [1]
()
LXRβ [1]
()
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[1].

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[2].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 88 mg/mL
(200.19 mM)


* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 439.57
Formula

C24H29N3O3S

CAS No. 898800-26-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C)N1C(=O)C(=C(S1(=O)=O)C2=CC=CC=C2)NC3=CC=C(C=C3)N4CCCCC4

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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