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.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 506.5. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.97 mL||9.87 mL||19.74 mL|
|5 mM||0.39 mL||1.97 mL||3.95 mL|
|10 mM||0.2 mL||0.99 mL||1.97 mL|
|50 mM||0.04 mL||0.2 mL||0.39 mL|
References are publications that support the products' biological activity.
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 PMID: 7731010
Jones et al (1999) The effect of the endothelin ETA receptor antagonist CI-1020 on hypoxic pulmonary vasoconstriction. Eur.J.Pharmacol. 374 367 PMID: 10422781
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 PMID: 12130731
If you know of a relevant reference for CI 1020, please let us know.
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Keywords: CI 1020, supplier, selective, orally, active, ETA, antagonists, Receptors, Endothelin, CI1020, Pfizer, PD156707, PD, 156707, Endothelin, ETA, Receptors, Endothelin, ETA, Receptors, Tocris Bioscience
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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.