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Darusentan

Names

[ CAS No. ]:
171714-84-4

[ Name ]:
Darusentan

[Synonym ]:
Benzenepropanoic acid, α-[(4,6-dimethoxy-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-, (αS)-
(+)-(S)-2-(4,6-dimethoxypyrimidine-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid
(2S)-2-[(4,6-dimethoxypyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid
HMR-4005
henyl-,(S)
Darusentan
(+)-(S)-2-(4,6-dimethoxy-pyrimidin-2-yloxy)-3-methoxy-3,3-diphenyl-propionic acid
(2S)-2-[(4,6-Dimethoxy-2-pyrimidinyl)oxy]-3-methoxy-3,3-diphenylpropanoic acid

Biological Activity

[Description]:

Darusentan is a selective endothelin A (ETA) receptor antagonist. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM[1].

[Related Catalog]:

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

[References]

[1]. Liang F, et al. Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries. Can J Physiol Pharmacol. 2010 Aug;88(8):840-9.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
587.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H22N2O6

[ Molecular Weight ]:
410.420

[ Flash Point ]:
309.0±32.9 °C

[ Exact Mass ]:
410.147797

[ PSA ]:
100.00000

[ LogP ]:
6.90

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.583

Safety Information

[ Hazard Codes ]:
Xn

Related Compounds