Nebentan potassium  (Synonyms: YM598)

Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ET_A receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [¹²⁵I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with K_i of 0.697 nM and 569 nM, respectively^[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo^[2].

Nebentan potassium inhibits the specific binding of [¹²⁵I] endothelin-1 to endothelin ET_A and ET_B receptors in a concentration dependent manner, K_i values are 0.697 nM and 1.53 nM for human and rat endothelin ETA receptors, respectively. In contrast, YM598 exhibits low affinities for human and rat endothelin ET_B receptors, with K_i values of 569 nM and 155 nM,respectively^[1].
In measurement of intracellular Ca²⁺ concentration, Nebentan potassium concentration-dependently inhibits the increase in [Ca²⁺]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC₅₀ values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Nebentan potassium (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 potassium (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

529.61

Solid

C₂₄H₂₀KN₅O₅S

342005-82-7

O=S(/C=C/C1=CC=CC=C1)([N-]C2=NC(C3=NC=CC=N3)=NC(OC)=C2OC4=CC=CC=C4OC)=O.[K+]

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [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:  [Content Brief]