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Nebentan

CAT: 0804-HY-106994Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-106994Size:1 Each
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Description
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan. 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].
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.
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