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Avosentan

Names

[ CAS No. ]:
290815-26-8

[ Name ]:
Avosentan

[Synonym ]:
Avosentan
UNII-L94KSX715K
2-Pyridinesulfonamide, N-[6-methoxy-5-(2-methoxyphenoxy)-2-(4-pyridinyl)-4-pyrimidinyl]-5-methyl-
N-[6-Methoxy-5-(2-methoxyphenoxy)-2-(4-pyridinyl)-4-pyrimidinyl]-5-methyl-2-pyridinesulfonamide
Ro 67-0565
SPP301

Biological Activity

[Description]:

Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.IC50 value:Target: ETA receptor

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor
Research Areas >> Cardiovascular Disease

[References]

[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]. Mann JF, Green D, Jamerson K, Ruilope LM, Kuranoff SJ, Littke T, Viberti G; ASCEND Study Group. J Am Soc Nephrol. 2010 Mar;21(3):527-35.

[4]. Dieterle W, Hengelage T. Absolute bioavailability and pharmacokinetics of avosentan in man. Int J Clin Pharmacol Ther. 2009 Sep;47(9):587-94.

[5]. 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.


[Related Small Molecules]

BQ-788 (sodium salt) | Endothelin-1 (human, bovine, dog, mouse, porcine, rat) acetate salt | Atrasentan hydrochloride | BQ-123 | Zibotentan (ZD4054) | ACT-132577 | RE 201 | Atrial Natriuretic Factor (1-28) (mouse, rabbit, rat) trifluoroacetate salt | Sitaxentan sodium | IRL-1620 TFA | Sulfisoxazole | Aminaftone | PD-159020 | Ro 46-2005 | ZD-1611

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
575.5±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H21N5O5S

[ Molecular Weight ]:
479.508

[ Flash Point ]:
301.8±32.9 °C

[ Exact Mass ]:
479.126343

[ PSA ]:
133.80000

[ LogP ]:
0.87

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.621

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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