AZ876

Names

[ Name ]:
AZ876

[Synonym ]:
MFCD30377191
AZ12260493
2-(2-Methyl-2-propanyl)-5-phenyl-4-{[4-(1-piperidinyl)phenyl]amino}-1,2-thiazol-3(2H)-one 1,1-dioxide
3(2H)-Isothiazolone, 2-(1,1-dimethylethyl)-5-phenyl-4-[[4-(1-piperidinyl)phenyl]amino]-, 1,1-dioxide

Biological Activity

[Description]:

AZ876 is a novel high-affinity LXR agonist. AZ876 was 25-fold and 2.5-fold more potent than GW3965 (HY-10627) on human (h)LXRα and hLXRβ respectively.(1) AZ876 suppressed up-regulation of hypertrophy- and fibrosis-related genes, and further inhibited prohypertrophic and profibrotic transforming growth factor β (TGFβ)-Smad2/3 signalling.(2) AZ876 prevented TGFβ- and angiotensin II-induced fibroblast collagen synthesis, and inhibited up-regulation of the myofibroblastic marker, α-smooth muscle actin.(3) The reference for administration is 20 umol/kg/day in vivo.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> LXR

Research Areas >> Cancer

[References]

[1]. Cannon MV et al. 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.

[2]. van der Hoorn J et al. 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.

[Related Small Molecules]

T0901317 | GW3965 HCl | WAY 252623 | SR 9243 | (20S)-Protopanaxatriol | 27-Hydroxycholesterol | GSK 2033 | SR 9238 | 24-Hydroxycholesterol | BMS-779788 | BMS-852927 | Nagilactone B | RGX-104 | Rovazolac

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
605.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₉N₃O₃S

[ Molecular Weight ]:
439.570

[ Flash Point ]:
319.9±34.3 °C

[ Exact Mass ]:
439.192963

[ LogP ]:
3.27

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.642

[ Storage condition ]:
2-8℃