290815-26-8
Chemical Structure
Avosentan
Synonym(s): Ro 67-0565; SPP-301
- CAS 番号: 290815-26-8
- Formula:C23H21N5O5S
- Molecular Weight:479.51
IUPAC Name: N-(6-methoxy-5-(2-methoxyphenoxy)-2-(pyridin-4-yl)pyrimidin-4-yl)-5-methylpyridine-2-sulfonamide
InChIKey: YBWLTKFZAOSWSM-UHFFFAOYSA-N
SMILES: COC1=C(OC(C(NS(C2=NC=C(C=C2)C)(=O)=O)=NC(C3=CC=NC=C3)=N4)=C4OC)C=CC=C1
Biological Activity: Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure[1][2][3][4].
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Avosentan | 98.15% | Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure. | ||||||||||||||||||||
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Avosentan (Standard) | ≥98% | Avosentan (Standard) is the analytical standard of Avosentan (HY-15195). This product is intended for research and analytical applications. Avosentan is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction, and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure. | ||||||||||||||||||||
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- [1]. Baltatu OC, Iliescu R, Zaugg CE, Reckelhoff JF, Louie P, Schumacher C, Campos LA. Antidiuretic effects of the endothelin receptor antagonist avosentan. Front Physiol. 2012;3:103. [Content Brief]
- [2]. Konieczka K, Meyer P, Schoetzau A, Neutzner A, Mozaffarieh M, Flammer J. Effect of avosentan (SPP-301) in porcine ciliary arteries. Curr Eye Res. 2011 Feb;36(2):118-24. [Content Brief]
- [3]. Baltatu OC, et al. Avosentan is protective in hypertensive nephropathy at doses not causing fluid retention. Pharmacol Res. 2014 Feb;80:9-13. [Content Brief]
- [4]. Effect of SPP 301, an Endothelin Antagonist, on Intraocular Pressure in Glaucomatous Monkey Eyes By Wang, Rong-Fang; Podos, Steven M.; Serle, Janet B.; Baltatu, Ovidiu C. From Current Eye Research (2011), 36(1), 41-46.
Keywords
