Name | ZD-1611 |
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Synonyms |
3-(4-{3-[(3-Methoxy-5-methyl-2-pyrazinyl)sulfamoyl]-2-pyridinyl}phenyl)-2,2-dimethylpropanoic acid
Benzenepropanoic acid, 4-[3-[[(3-methoxy-5-methyl-2-pyrazinyl)amino]sulfonyl]-2-pyridinyl]-α,α-dimethyl- |
Description | ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke. |
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Related Catalog | |
In Vitro | ZD1611 competitively inhibits 125I-labeled ET-1 binding at human cloned ETA and ETB receptors with pIC50 values of 8.6 and 5.6, respectively, showing 1000-fold selectivity for the ETA receptor[1]. |
In Vivo | ZD1611 (0.3 mg/kg, p.o.) has a duration of action of more than 7 h in rats. In the dog, ZD1611 is active for at least 6 h at dose of 0.6 mg/kg p.o[1]. ZD1611 (0.15 mg/kg/day) in combination with candesartan decreases the brain damage and improves the neurological scores in rats. However, ZD1611 or candesartan alone does not significantly decrease the brain damage or improve neurological scores[2]. |
Animal Admin | The precursor of ET-1, big ET-1, is used for in vivo analysis of the effects of ZD1611. Exogenously administered big ET-1 is converted to the biologically active peptide ET-1 in vivo via a phosphoramidon-sensitive ET-converting enzyme. In the present study, the use of big ET-1 in vivo is preferred because this compound fails to elicit the initial depressor response associated with i.v. administered ET-1 and yields a greater maximum response than that to ET-1 itself. A partial cumulative dose-response curve to i.v. big ET-1 starting at 0.3 nmol/kg) is constructed until pressor responses >30 mm Hg are achieved. After a 55-min recovery period, ZD1611 (0.03-0.3 mg/kg) or vehicle is administered, and the big ET-1-response curve is repeated 5 min later. The activity of ZD1611 is calculated as a ratio of the dose of big ET-1 required to give a 30-mm Hg rise in MAP in the absence and then the presence of the compound. |
References |
Density | 1.3±0.1 g/cm3 |
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Boiling Point | 653.9±65.0 °C at 760 mmHg |
Molecular Formula | C22H24N4O5S |
Molecular Weight | 456.515 |
Flash Point | 349.3±34.3 °C |
Exact Mass | 456.146729 |
LogP | 3.71 |
Vapour Pressure | 0.0±2.1 mmHg at 25°C |
Index of Refraction | 1.608 |
Storage condition | 2-8℃ |