Nebentan potassium - 10mM in DMSO , CAS No.342005-82-7

CAS: 342005-82-7 Cat. No.: N654865 Formule: C₂₄H₂₀KN₅O₅S Poids moléculaire: 529.61 PubChem CID: 12093171

GRADE & PURITY 10mM in DMSO

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Vue d’ensemble

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

In Vitro

Nebentan potassium inhibits the specific binding of [ 125 I] 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. In measurement of intracellular Ca 2+ concentration, Nebentan potassium concentration-dependently inhibits the increase in [Ca 2+ ]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC 50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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

IC50& Target:ET A 0.679 nM (Ki) ET B 569 nM (Ki)

Specifications

Spécifications et pureté

10mM in DMSO

Mécanismes biochimiques et physiologiques

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 [ 125 I] endothelin-1 binding to cloned human endothelin ETA

Conditions de stockage de stockage

Desiccated,Store at -80°C

Expédié en

Dry ice packs + Cold packs

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

ANTAGONIST

Noms et identifiants

Isomères SMILES

COC1=CC=CC=C1OC2=C(N=C(N=C2OC)C3=NC=CC=N3)[N-]S(=O)(=O)/C=C/C4=CC=CC=C4.[K+]

CAS alternatif

342005-82-7

PubChem CID

12093171

Termes d'entrée MeSH

N-(6-methoxy-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl)-2-phenylethenesulfonamide;N-MMPP-phenylethenesulfonamide;YM-598;YM598

Poids moléculaire

529.61

Foire aux questions

How should this product be stored?

Store at ?80 °C, desiccated. Keep the container tightly closed with desiccant — the material is moisture-sensitive.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 342005-82-7, the molecular formula is C24H20KN5O5S, and the molecular weight is 529.61 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.