162256-50-0
Chemical Structure
CI-1020
Synonym(s): PD156707
- CAS No.: 162256-50-0
- Formula:C28H26O9
- Molecular Weight:506.50
IUPAC Name: 3-(benzo[d][1,3]dioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-(3,4,5-trimethoxybenzyl)furan-2(5H)-one
InChIKey: PWIPORDFWDZCJG-UHFFFAOYSA-N
SMILES: O=C1OC(C2=CC=C(OC)C=C2)(O)C(CC3=CC(OC)=C(OC)C(OC)=C3)=C1C4=CC=C(OCO5)C5=C4
Biological Activity: 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].
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CI-1020 | 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. | |||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Doherty AM, et al. Discovery and development of an endothelin A receptor-selective antagonist PD 156707. Pharm Biotechnol. 1998;11:81-112. [Content Brief]
- [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. [Content Brief]
Keywords
