Avosentan

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].

Product Specifications

CAS Number

[290815-26-8]

Product Name Alternative

Ro 67-0565; SPP-301

UNSPSC

12352005

Hazard Statement

H315, H319, H335, H413

Target

Endothelin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Endocrinology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/avosentan.html

Concentration

10mM

Purity

98.15

Solubility

DMSO : 6.67 mg/mL (ultrasonic)

Smiles

COC1=C(OC(C(NS(C2=NC=C(C=C2)C)(=O)=O)=NC(C3=CC=NC=C3)=N4)=C4OC)C=CC=C1

Molecular Formula

C23H21N5O5S

Molecular Weight

479.51

Precautions

H315, H319, H335, H413

References & Citations

[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.|[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.|[3]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.|[4]Baltatu OC, et al. Avosentan is protective in hypertensive nephropathy at doses not causing fluid retention. Pharmacol Res. 2014 Feb;80:9-13.