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PD-159020

Names

[ CAS No. ]:
177904-00-6

[ Name ]:
PD-159020

[Synonym ]:
1H-Indole-2-carboxylic acid, 3-(1,3-benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-5-methoxy-6-(phenylmethoxy)-
3-(1,3-Benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-6-(benzyloxy)-5-methoxy-1H-indole-2-carboxylic acid

Biological Activity

[Description]:

PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively.

[Related Catalog]:

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

[Target]

IC50: 30 nM (hETA), 50 nM (hETB)[1]


[In Vitro]

PD-159020 demonstrates excellent inhibition of arachidonic acid release, AAR-B, with an IC50 of 0.23 μM.

[References]

[1]. Amy Mbunker, et al. 1,3-diaryl-2-carboxyindoles as potent non-peptide endothelin antagonists. Bioorganic & Medicinal Chemistry Letters. Volume 6, Issue 9, 7 May 1996, Pages 1061-1066


[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 | Ro 46-2005 | ZD-1611

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
758.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C32H25NO8

[ Molecular Weight ]:
551.543

[ Flash Point ]:
412.4±32.9 °C

[ Exact Mass ]:
551.158020

[ LogP ]:
5.92

[ Vapour Pressure ]:
0.0±2.7 mmHg at 25°C

[ Index of Refraction ]:
1.670

[ Storage condition ]:
2-8℃

Related Compounds