Cas No.: | 898800-26-5 |
Chemical Name: | 2-Tert-Butyl-5-phenyl 4-[(4-piperidin-1-ylphenyl)amino]isothiazol-3(2H)-one 1,1-dioxide |
Synonyms: | AZ876;AZ-876;AZ12260493;AZ 876;2-(1,1-Dimethylethyl)-5-phenyl-4-[[4-(1-piperidinyl)phenyl]amino]-3(2H)-isothiazolone 1,1-dioxide;AZ 12260493;GTPL7725;BCP19166;s6427;Q27074652;2-tert-butyl-1,1-dioxo-5-phenyl-4-(4-piperidin-1-ylanilino)-1,2-thiazol-3-one;2-tert-butyl-1,1-dioxo-5-phenyl-4-[(4-piperidin-1-ylphenyl)amino]-1,2-thiazol-3-one;2-tert-Butyl-5-pheny 4-[(4-piperidin-1-ylphenyl)amino]isothia;2-Tert-Butyl-5-phenyl 4-[(4-piperidin-1-ylphenyl)amino]isothiazol-3(2H)-one 1,1-dioxide |
SMILES: | S1(C(C2C([H])=C([H])C([H])=C([H])C=2[H])=C(C(N1C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O)N([H])C1C([H])=C([H])C(=C([H])C=1[H])N1C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])(=O)=O |
Formula: | C24H29N3O3S |
M.Wt: | 439.5704 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |
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. |