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

AZ876
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526922

CAS#: 898800-26-5

Description: 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

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526922
Name: AZ876
CAS#: 898800-26-5
Chemical Formula: C24H29N3O3S
Exact Mass: 439.19
Molecular Weight: 439.574
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	Ready to ship
50mg	USD 250	Ready to ship
100mg	USD 450	Ready to ship
200mg	USD 750	Ready to ship
500mg	USD 1650	Ready to ship
1g	USD 2950	Ready to ship
2g	USD 5250	Ready to ship
5g	USD 9650	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	dmso	94.0	213.84

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. 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.

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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.

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