Nebentan

• Description :

  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].

• Product Name Alternative :

  YM598 (free base)

• UNSPSC :

  12352005

• Target :

  Endothelin Receptor

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Inflammation/Immunology; Cardiovascular Disease; Cancer

• Assay Protocol :

  https://www.medchemexpress.com/nebentan-free-base.html

• Purity :

  99.67

• Solubility :

  DMSO : 125 mg/mL (ultrasonic)

• Smiles :

  O=S(/C=C/C1=CC=CC=C1)(NC2=NC(C3=NC=CC=N3)=NC(OC)=C2OC4=CC=CC=C4OC)=O

• Molecular Formula :

  C24H21N5O5S

• Molecular Weight :

  491.52

• References & Citations :

  [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.|[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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  ETA; ETB

• CAS Number :

  [403604-85-3]