Identification | Back Directory | [Name]
E 4177 | [CAS]
135070-05-2 | [Synonyms]
E 4177 2-[4-[(2-cyclopropyl-7-methylimidazo[4,5-b]pyridin-3-yl)methyl]phenyl]benzoic acid | [Molecular Formula]
C24H21N3O2 | [MDL Number]
MFCD00900702 | [MOL File]
135070-05-2.mol | [Molecular Weight]
383.449 |
Hazard Information | Back Directory | [Description]
E-4177 is an angiotensin type 1 receptor antagonist potentially for the treatment of hypertension. In rat adrenal cortex and liver, E4177 competitively inhibited the specific binding of 125I-[Sar1,Ile8]Ang II, with IC50 being (5.2 +/- 1.0) x 10(-8) M for the adrenal cortex and (1.2 +/- 0.3) x 10(-7) M for the liver. These IC50 values were similar to those for losartan, which showed an IC50 of (6.0 +/- 0.9) x 10(-8) M for the adrenal cortex and (1.3 +/- 0.5) x 10(-7) M for the liver. E4177 is a potent AT1 Ang II-receptor antagonist that may be clinically useful for the treatment of cardiovascular diseases such as hypertension. | [Uses]
E4177 (57G709) is an orally active angiotensin II receptor antagonist. E4177 can inhibit the growth of vascular smooth muscle cells (HASMC) and the increase of cell surface area. In addition, E4177 can also increase the expression of platelet-derived growth factor (PDGF) receptor. E4177 can be used in the study of vascular diseases[1]. | [References]
[1] Kuma S, et al. ANGIOTENSIN II‐INDUCED GROWTH OF VASCULAR SMOOTH MUSCLE CELLS IS ASSOCIATED WITH MODULATION OF CELL SURFACE AREA AND PLATELET‐DERIVED GROWTH FACTOR RECEPTOR EXPRESSION[J]. Clinical and experimental pharmacology and physiology, 2007, 34(3): 153-160. |
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