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Category:
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7TM Receptors Peptides (Cardiovascular)Endothelin ReceptorsET-A Receptor Compounds
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Cat.No.
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Product Name
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2942 |
CI 1020
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| Alternative name(s): |
PD
156707 |
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Price and Availability
Click here for full price details of
CI 1020
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Chemical Name:
3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-
4-[(3,4,5-trimethoxyphenyl)methyl]-2(5H)-furanone |
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Biological Activity:
Highly selective, orally active, non-peptide
endothelin-A receptor (ETA) antagonist (IC50 values are
0.3 and 480 nM for ETA and ETB receptors respectively).
Antihypertensive; blocks ET-1-induced pressor responses following oral
administration.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Doherty et al
(1995) Discovery of a novel series of orally active non-peptide endothelin-A
(ETA) receptor-selective antagonists. J.Med.Chem. 38
1259. Jones et al (1999) The effect of the endothelin ETA
receptor antagonist CI-1020 on hypoxic pulmonary vasoconstriction.
Eur.J.Pharmacol. 374 367. Coe et al (2002) The
endothelin A receptor antagonists PD 156707 (CI-1020) and PD 180988 (CI-1034)
reverse the hypoxic pulmonary vasoconstriction in ther perinatal lamb.
J.Pharmacol.Exp.Ther. 302 672.
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Keywords: CI 1020, Peptides (Cardiovascular), Highly Selective, Orally Active ETA Antagonist, PD 156707, CI1020, Tocris Bioscience
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