| Identification | Back Directory | [Name]
1-(1-(3-ethoxyphenyl)propyl)-7-(pyrimidin-5-ylmethoxy)-4,5-dihydro-1H-benzo[g]indazole-3-carboxylic acid | [CAS]
219705-77-8 | [Synonyms]
ATZ-1993
1-(1-(3-ethoxyphenyl)propyl)-7-(pyrimidin-5-ylmethoxy)-4,5-dihydro-1H-benzo[g]indazole-3-carboxylic acid
1H-Benz[g]indazole-3-carboxylic acid, 1-[1-(3-ethoxyphenyl)propyl]-4,5-dihydro-7-(5-pyrimidinylmethoxy)- | [Molecular Formula]
C28H28N4O4 | [MOL File]
219705-77-8.mol | [Molecular Weight]
484.55 |
| Hazard Information | Back Directory | [Uses]
ATZ-1993 is an orally active, nonpeptide endothelin receptor subtype Aand endothelin receptor subtype B antagonist with pKi values of 8.69, 7.20, respectively. ATZ-1993 has the potential for the research of intimal hyperplasia after balloon denudation of the carotid artery[1]. | [in vivo]
ATZ-1993 (30 mg/kg; drinking water, daily for 1 week) inhibits the intimal hyperplasia intimal hyperplasia after balloon denudation[1]. | Animal Model: | Japanese White male rabbits[1] | | Dosage: | 30 mg/kg | | Administration: | Drinking water, daily for 1 weeks | | Result: | Inhibited the intimal hyperplasia with the inhibition rate approximately 77%, increased in intima:media ratio and DNA content. |
| [IC 50]
ETA: 8.69 (pKi); ETB: 7.20 (pKi) | [References]
[1] Azuma H, et al. ATZ1993, an orally active and novel nonpeptide antagonist for endothelin receptors and inhibition of intimal hyperplasia after balloon denudation of the rabbit carotid artery. Jpn J Pharmacol. 1999 Sep;81(1):21-8. DOI:10.1254/jjp.81.21 |
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