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Ro 46-2005

Names

[ CAS No. ]:
150725-87-4

[ Name ]:
Ro 46-2005

[Synonym ]:
Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(3-methoxyphenoxy)-4-pyrimidinyl]-
N-[6-(2-Hydroxyethoxy)-5-(3-methoxyphenoxy)-4-pyrimidinyl]-4-(2-methyl-2-propanyl)benzenesulfonamide
Ro 46-2005
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(3-methoxyphenoxy)pyrimidin-4-yl]benzenesulfonamide

Biological Activity

[Description]:

Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.IC50 value: 220 nM (ETA) [2]Target: Endothelinin vitro: Ro 46-2005 proves to be equipotent (IC50 200-500 nM) for inhibition of [125I]ET-1 binding on the two known ET receptor subtypes (ETA and ETB). Ro 46-2005 also inhibits the functional consequences of ET-1 stimulation: the ET-l-induced release of arachidonic acid from rat mesangial cells was inhibited with an IC50 of 1.8 μM.[1]

[Related Catalog]:

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

[References]

[1]. Breu V, et al. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETBreceptors. FEBS Lett. 1993 Nov 15;334(2):210-214.

[2]. Clozel M, et al. Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature. 1993 Oct 21;365(6448):759-761.

[3]. N.R. Sibson, et al. MRI Determination of the Mechanisms Underlying TNF-a-induced Changes in Cerebral Blood Volume, Tissue Water Diffusion and BBB Permeability. Proc. Intl. Soc. Mag. Reson. Med. 10 (2002)


[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 | Avosentan | Sitaxentan sodium | IRL-1620 TFA | Sulfisoxazole | Aminaftone | PD-159020 | ZD-1611

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
617.5±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C23H27N3O6S

[ Molecular Weight ]:
473.542

[ Flash Point ]:
327.3±34.3 °C

[ Exact Mass ]:
473.162048

[ PSA ]:
128.25000

[ LogP ]:
2.22

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.593

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds