Nebentan

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 Specifications

CAS Number

[403604-85-3]

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.