AZ876 | AZ 876 | CAS#898800-26-5 | liver X receptor agonist

MedKoo Cat#: 526922 | Name: AZ876

Description:

WARNING: This product is for research use only, not for human or veterinary use.

AZ876, also known as AZ-876, is a liver X receptor agonist. AZ876 protects against pathological cardiac hypertrophy and fibrosis without lipogenic side effects. LXR activation with AZ876 attenuated this increase, and significantly reduced TAC-induced increases in heart weight, myocardial fibrosis, and cardiac dysfunction without affecting blood pressure. Liver X receptors (LXRs) transcriptionally regulate inflammation, metabolism, and immunity.

Chemical Structure

AZ876

CAS#898800-26-5

Theoretical Analysis

MedKoo Cat#: 526922

Name: AZ876

CAS#: 898800-26-5

Chemical Formula: C24H29N3O3S

Exact Mass: 439.1930

Molecular Weight: 439.57

Elemental Analysis: C, 65.58; H, 6.65; N, 9.56; O, 10.92; S, 7.29

Price and Availability

Size	Price	Availability
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 750.00	Ready to ship
500mg	USD 1,650.00	Ready to ship
1g	USD 2,950.00	Ready to ship
2g	USD 5,250.00	Ready to ship
5g	USD 9,650.00	Ready to ship

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Related CAS #

No Data

Synonym

AZ876; AZ 876; AZ-876, AZ12260493; AZ 12260493; AZ-12260493.

IUPAC/Chemical Name

2-(1,1-Dimethylethyl)-5-phenyl-4-[[4-(1-piperidinyl)phenyl]amino]-3(2H)-isothiazolone 1,1-dioxide

InChi Key

IVANYIPLGFVBGR-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H29N3O3S/c1-24(2,3)27-23(28)21(22(31(27,29)30)18-10-6-4-7-11-18)25-19-12-14-20(15-13-19)26-16-8-5-9-17-26/h4,6-7,10-15,25H,5,8-9,16-17H2,1-3H3

SMILES Code

O=C(C(NC1=CC=C(N2CCCCC2)C=C1)=C3C4=CC=CC=C4)N(C(C)(C)C)S3(=O)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot# A9T08K29

QC Data

View QC data: current batch, Lot# A9T08K29

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

AZ876 is a potent and high-affinity LXR agonist.

In vitro activity:

TBD

In vivo activity:

This study demonstrates that chronic administration of the LXR agonist AZ876 attenuated pathological cardiac hypertrophy in a murine model of chronic pressure overload without altering systemic blood pressure, implicating heart-specific effects. AZ876 treatment diminished myocardial fibrosis and suppressed induction of profibrotic gene expression. At the cellular level, both cardiac myocytes and fibroblasts, the two major cell types in the heart, expressed LXRs, and, furthermore, these cells were direct targets in AZ876-mediated cellular protection from hypertrophic and fibrotic stimuli. Overall, the salutary effects of AZ876 on cardiac remodelling were associated with a trend toward an improved functional outcome, which, importantly, occurred in the absence of adverse lipogenic side effects typical of current LXR agonists such as T09 and GW3965. Reference: Eur J Heart Fail. 2015 Mar;17(3):273-82. https://onlinelibrary.wiley.com/doi/full/10.1002/ejhf.243

	Solvent	mg/mL	mM
Solubility
	dmso	94.0	213.84

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 439.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. van der Hoorn J, Lindén D, Lindahl U, Bekkers M, Voskuilen M, Nilsson R, Oscarsson J, Lindstedt E, Princen H. Low dose of the liver X receptor agonist, AZ876, reduces atherosclerosis in APOE*3Leiden mice without affecting liver or plasma triglyceride levels. Br J Pharmacol. 2011 Apr;162(7):1553-63. doi: 10.1111/j.1476-5381.2010.01168.x. PMID: 21175581; PMCID: PMC3057293. 2. Cannon MV, Yu H, Candido WM, Dokter MM, Lindstedt EL, Silljé HH, van Gilst WH, de Boer RA. The liver X receptor agonist AZ876 protects against pathological cardiac hypertrophy and fibrosis without lipogenic side effects. Eur J Heart Fail. 2015 Mar;17(3):273-82. doi: 10.1002/ejhf.243. Epub 2015 Feb 11. PMID: 25684370.

In vitro protocol:

TBD

In vivo protocol:

1: Cannon MV, Yu H, Candido WM, Dokter MM, Lindstedt EL, Silljé HH, van Gilst WH, de Boer RA. The liver X receptor agonist AZ876 protects against pathological cardiac hypertrophy and fibrosis without lipogenic side effects. Eur J Heart Fail. 2015 Mar;17(3):273-82. doi: 10.1002/ejhf.243. Epub 2015 Feb 11. PubMed PMID: 25684370. 2: van der Hoorn J, Lindén D, Lindahl U, Bekkers M, Voskuilen M, Nilsson R, Oscarsson J, Lindstedt E, Princen H. Low dose of the liver X receptor agonist, AZ876, reduces atherosclerosis in APOE*3Leiden mice without affecting liver or plasma triglyceride levels. Br J Pharmacol. 2011 Apr;162(7):1553-63. doi: 10.1111/j.1476-5381.2010.01168.x. PubMed PMID: 21175581; PubMed Central PMCID: PMC3057293.