Nebentan - 10mM in DMSO , Endothelin receptor ET-A antagonist, CAS No.403604-85-3, Endothelin receptor ET-A antagonist

CAS: 403604-85-3 Cat. No.: N654496 Formula: C₂₄H₂₁N₅O₅S Peso molecolare: 491.52 PubChem CID: 9957262

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ET A receptor antagonist through the modification of Bosentan . Nebentan 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 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 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 (oral administration; 0.1-1 mg/kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy. Nebentan (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 0.697 nM (Ki) ET B 569 nM (Ki)

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ET A receptor antagonist through the modification of Bosentan ( HY-A0013 ). Nebentan inhibits [ 125 I] endothelin-1 binding to cloned human endothelin ETA and ETB r

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

ANTAGONIST

Meccanismo d'azione

Endothelin receptor ET-A antagonist

Proprietà del prodotto

• ALogP: 3.3

Nomi e identificatori

• Isomeri SMILES: COC1=CC=CC=C1OC2=C(N=C(N=C2OC)C3=NC=CC=N3)NS(=O)(=O)/C=C/C4=CC=CC=C4
• CAS alternativo: 403604-85-3
• PubChem CID: 9957262
• Peso molecolare: 491.52

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

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 403604-85-3, the molecular formula is C24H21N5O5S, and the molecular weight is 491.52 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.