Elsibucol - CAS 216167-95-2
Catalog number: 216167-95-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C35H54O4S2
Molecular Weight:
602.94
COA:
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Targets:
Others
Description:
Elsibucol, a metabolically stable derivative of probucol, inhibits atherosclerosis and preserves endothelial healing following arterial injury. In vitro, elsibucol reduces vascular smooth muscle cell proliferation without affecting cell viability.
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Purity:
>98%
Appearance:
Solid powder
Synonyms:
4-[2,6-ditert-butyl-4-[2-(3,5-ditert-butyl-4-hydroxyphenyl)sulfanylpropan-2-ylsulfanyl]phenoxy]butanoic acid; (4,2,6-di-tert-butyl-4-(1-(3,5-di-tert-butyl-4-hydroxy-phenylsulfanyl)-1-methyl-ethylsulfanyl)-phenoxy-butyric acid); AGI-1096; elsibucol
MSDS:
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InChIKey:
YHFUPQNXMNMQAK-UHFFFAOYSA-N
InChI:
1S/C35H54O4S2/c1-31(2,3)24-18-22(19-25(29(24)38)32(4,5)6)40-35(13,14)41-23-20-26(33(7,8)9)30(27(21-23)34(10,11)12)39-17-15-16-28(36)37/h18-21,38H,15-17H2,1-14H3,(H,36,37)
Canonical SMILES:
CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)SC(C)(C)SC2=CC(=C(C(=C2)C(C)(C)C)OCCCC(=O)O)C(C)(C)C
1.Lead acetate induces EGFR activation upstream of SFK and PKCalpha linkage to the Ras/Raf-1/ERK signaling.
Wang CY1, Wang YT, Tzeng DW, Yang JL. Toxicol Appl Pharmacol. 2009 Mar 1;235(2):244-52. doi: 10.1016/j.taap.2008.12.007. Epub 2008 Dec 24.
Lead acetate (Pb), a probable human carcinogen, can activate protein kinase C (PKC) upstream of extracellular signal-regulated kinase 1 and 2 (ERK1/2). Yet, it remains unclear whether Pb activation of PKC --> ERK1/2 involves receptor/non-receptor tyrosine kinases and the Ras signaling transducer. Here we demonstrate a novel mechanism elicited by Pb for transmitting ERK1/2 signaling in CL3 human non-small-cell lung adenocarcinoma cells. Pb induction of higher steady-state levels of Ras-GTP was essential for increasing phospho-Raf-1(S338) and phospho-ERK1/2. Pre-treatment of the cells with a conventional PKC inhibitor Gö6976 or depleting PKCalpha using specific small interfering RNA blocked Pb induction of Ras-GTP. Pb also activated cellular tyrosine kinases. Specific pharmacological inhibitors, PD153035 for epidermal growth factor receptor (EGFR) and SU6656 for Src family tyrosine kinases (SFK), but not AG1296 for platelet-derived growth factor receptor, could suppress the Pb-induced tyrosine kinases, PKCalpha, Ras-GTP, phospho-Raf-1(S338) and phospho-ERK1/2.
2.Effects of AGI-1096, a novel antioxidant compound with anti-inflammatory and antiproliferative properties, on rodent allograft arteriosclerosis.
Murata S1, Sundell CL, Lijkwan MA, Balsam LB, Hammainen P, Coleman C, York C, Luchoomun J, Suen KL, Howard R, Somers PK, Morris RE, Robbins RC. Transplantation. 2004 May 27;77(10):1494-500.
BACKGROUND: AGI-1096 is a novel phenolic intracellular antioxidant with anti-inflammatory and antiproliferative properties. In vitro, AGI-1096 inhibited the inducible expression of vascular cell adhesion molecule (VCAM)-1, E-selectin, and monocyte chemoattractant protein (MCP)-1 in endothelial cells and tumor necrosis factor (TNF)-alpha and interleukin (IL)-1beta secretion from lipopolysaccharide (LPS)-stimulated peripheral blood mononuclear cells. It also inhibited serum-stimulated proliferation of aortic smooth-muscle cells. In vivo, AGI-1096 demonstrated anti-inflammatory properties in a murine delayed-type hypersensitivity model. Given these antioxidant, anti-inflammatory and antiproliferative properties, we reasoned that AGI-1096 may be able to prevent chronic allograft arteriosclerosis. This hypothesis was tested in a rodent aortic transplantation model.
3.Elsibucol inhibits atherosclerosis following arterial injury: multifunctional effects on cholesterol levels, oxidative stress and inflammation.
Dussault S1, Dhahri W1, Desjarlais M1, Mathieu R1, Rivard A2. Atherosclerosis. 2014 Nov;237(1):194-9. doi: 10.1016/j.atherosclerosis.2014.09.008. Epub 2014 Sep 16.
BACKGROUND: Elsibucol is a metabolically stable derivative of probucol with antioxidant, anti-inflammatory and antiproliferative properties. Here we investigated the effect of elsibucol on the development of atherosclerosis following arterial injury in hypercholesterolemic rabbits.
4.Helicobacter pylori seroprevalence in patients with chronic obstructive pulmonary disease and its relation to pulmonary function tests.
Gencer M1, Ceylan E, Yildiz Zeyrek F, Aksoy N. Respiration. 2007;74(2):170-5. Epub 2005 Dec 6.
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is a slowly progressive condition characterized by poorly reversible airflow limitation that is associated with an abnormal inflammatory response of the lung. It has been shown that there is a seroepidemiological association of Helicobacter pylori (Hp) infection with many inflammatory conditions.
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CAS 216167-95-2 Elsibucol

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