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RO 46-8443

Names

[ CAS No. ]:
175556-12-4

[ Name ]:
RO 46-8443

[Synonym ]:
Ro 46-8443
MFCD00946586
Benzenesulfonamide, N-[6-[(2R)-2,3-dihydroxypropoxy]-5-(2-methoxyphenoxy)-2-(4-methoxyphenyl)-4-pyrimidinyl]-4-(1,1-dimethylethyl)-
N-{6-[(2R)-2,3-Dihydroxypropoxy]-5-(2-methoxyphenoxy)-2-(4-methoxyphenyl)-4-pyrimidinyl}-4-(2-methyl-2-propanyl)benzenesulfonamide

Biological Activity

[Description]:

Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM)[1][2].

[Related Catalog]:

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

[Target]

ETB:34-69 nM (IC50)

ETA:6800 nM (IC50)


[References]

[1]. Breu V, et al. In vitro characterisation of Ro 46-8443, the first non-peptide antagonist selective for the endothelin ETB receptor. FEBS Lett. 1996;383(1-2):37-41.

[2]. Clozel M, et al. The role of ETB receptors in normotensive and hypertensive rats as revealed by the non-peptide selective ETB receptor antagonist Ro 46-8443. FEBS Lett. 1996;383(1-2):42-45.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
683.1±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H35N3O8S

[ Molecular Weight ]:
609.690

[ Flash Point ]:
367.0±34.3 °C

[ Exact Mass ]:
609.214478

[ LogP ]:
3.22

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.602

[ Storage condition ]:
2-8°C

Related Compounds