Ro 46-2005

Modify Date: 2024-01-16 11:47:48

Ro 46-2005 Structure
Ro 46-2005 structure
Common Name Ro 46-2005
CAS Number 150725-87-4 Molecular Weight 473.542
Density 1.3±0.1 g/cm3 Boiling Point 617.5±65.0 °C at 760 mmHg
Molecular Formula C23H27N3O6S Melting Point N/A
MSDS N/A Flash Point 327.3±34.3 °C

 Use of Ro 46-2005


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]

 Names

Name 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(3-methoxyphenoxy)pyrimidin-4-yl]benzenesulfonamide
Synonym More Synonyms

 Ro 46-2005 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
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)

 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

~%

Ro 46-2005 Structure

Ro 46-2005

CAS#:150725-87-4

Literature: Hoffmann-La Roche Inc. Patent: US5292740 A1, 1994 ; US 5292740 A

 Precursor & DownStream

Precursor  1

DownStream  0

 Synonyms

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