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CI-1020
SKU
HY-103459-Get quote
Category Reference compound
Tags Cardiovascular Disease, Endothelin Receptor, GPCR/G Protein
Products Details
Product 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].
Web ID
– HY-103459
Shipping
– Room temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C28H26O9
References
– [1]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.|[2]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.|[3]Doherty AM, et al. Discovery and development of an endothelin A receptor-selective antagonist PD 156707. Pharm Biotechnol. 1998;11:81-112. |[4]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.
CAS Number
– 162256-50-0
Molecular Weight
– 506.50
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
Clinical Information
– No Development Reported
Research Area
– Cardiovascular Disease
Solubility
– 10 mM in DMSO
Target
– Endothelin Receptor
Isoform
– ETA
Pathway
– GPCR/G Protein
Product type
– Reference compound
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