CI 1020

Names

[ Name ]:
CI 1020

[Synonym ]:
PPADS tetrasodium salt
CI 1020

Biological Activity

[Description]:

CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration[1][2][3].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor

[Target]

ETA:0.3 nM (IC50)

[References]

[1]. Maguire JJ, et al. ETA receptor antagonists inhibit intimal smooth muscle cell proliferation in human vessels. Clin Sci (Lond). 2002 Aug;103 Suppl 48:184S-188S.

[2]. Doherty AM, et al. Discovery and development of an endothelin A receptor-selective antagonist PD 156707. Pharm Biotechnol. 1998;11:81-112.

[3]. Jones RD, et al. The effect of the endothelin ET(A) receptor antagonist CI-1020 on hypoxic pulmonary vasoconstriction. Eur J Pharmacol. 1999 Jun 25;374(3):367-75.

[4]. Sheedy W, et al. The effect of the ETA receptor antagonist (CI-1020) in rats with established hypoxic pulmonary hypertension. Pulm Pharmacol Ther. 1998 Apr-Jun;11(2-3):173-6.

Chemical & Physical Properties

[ Density]:
1.351g/cm3

[ Boiling Point ]:
722.338ºC at 760 mmHg

[ Molecular Formula ]:
C₂₈H₂₆O₉

[ Molecular Weight ]:
506.50

[ Flash Point ]:
242.505ºC

[ Exact Mass ]:
506.15800

[ PSA ]:
101.91000

[ LogP ]:
3.84810

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.623

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds

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