| Identification | Back Directory | [Name]
Nebentan | [CAS]
403604-85-3 | [Synonyms]
Nebentan
Nebentan free base
Ethenesulfonamide, N-[6-methoxy-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]-2-phenyl-, (1E)- | [Molecular Formula]
C24H21N5O5S | [MDL Number]
MFCD12912486 | [MOL File]
403604-85-3.mol | [Molecular Weight]
491.52 |
| Hazard Information | Back Directory | [Uses]
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. | [in vivo]
Nebentan (oral administration; 0.1-1 mg/kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy[2].Nebentan (oral administration; 1 mg/kg; 30 weeks) significantly ameliorates the poor survival rate of CHF rats, it markedly reduces the hypertrophy of both ventricles as well as pulmonary congestion[2]. | [IC 50]
ETA: 0.697 nM (Ki); ETB: 569 nM (Ki) | [References]
[1] Hironori Yuyama, et al. Pharmacological Characterization of YM598, an Orally Active and Highly Potent Selective Endothelin ET(A) Receptor Antagonist. Eur J Pharmacol. 2003 Sep 30;478(1):61-71. DOI:10.1016/j.ejphar.2003.08.031
[2] Akira Fujimori, et al. YM598, an Orally Active ET(A) Receptor Antagonist, Ameliorates the Progression of Cardiopulmonary Changes and Both-Side Heart Failure in Rats With Cor Pulmonale and Myocardial Infarction. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S354-7. DOI:10.1097/01.fjc.0000166304.40937.0b |
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