162256-50-0

162256-50-0 structure

Name: CI 1020
Chemical Name: 3-(1,3-benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(3,4,5-trimethoxyphenyl)methyl]furan-2-one
CAS Number: 162256-50-0
Molecular Formula: C₂₈H₂₆O₉
Molecular Weight: 506.50
Catalog: Signaling Pathways GPCR/G Protein Endothelin Receptor
Create Date: 2017-01-29 03:09:31
Modify Date: 2024-01-09 18:22:42
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].

Name	3-(1,3-benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(3,4,5-trimethoxyphenyl)methyl]furan-2-one
Synonyms	PPADS tetrasodium salt CI 1020

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.

162256-48-6

162256-50-0

Literature: Journal of Medicinal Chemistry, , vol. 42, # 12 p. 2162 - 2168

120-57-0

162256-50-0

Literature: Journal of Medicinal Chemistry, , vol. 42, # 12 p. 2162 - 2168

86-81-7

162256-49-7

162256-50-0

Literature: Journal of Medicinal Chemistry, , vol. 38, # 8 p. 1259 - 1263

144309-50-2

162256-50-0

Literature: Journal of Medicinal Chemistry, , vol. 42, # 12 p. 2162 - 2168

Precursor 3
162256-48-6 120-57-0 86-81-7
DownStream 0