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Nebentan

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Catalog No. T36007Cas No. 403604-85-3

Nebentan (YM598) 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].

Nebentan

Nebentan

😃Good
Catalog No. T36007Cas No. 403604-85-3
Nebentan (YM598) 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].
Pack SizePriceAvailabilityQuantity
5 mg$197Backorder
10 mg$332Backorder
25 mg$581Backorder
1 mL x 10 mM (in DMSO)$224Backorder
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Product Introduction

Bioactivity
Description
Nebentan (YM598) 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].
Targets&IC50
ETB:569 nM (Ki), ETA:0.697 nM (Ki)
In vitro
Nebentan inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration-dependent manner, with Ki values of 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 ETB receptors, with Ki values of 569 nM and 155 nM, respectively [1]. Nebentan also inhibits the endothelin-1-induced increase in intracellular Ca2+ concentration ([Ca2+]i) in both CHO and A10 cells, with IC50 values of 26.2 nM and 26.7 nM, respectively [1].
In vivo
Nebentan, administered orally at dosages of 0.1-1 mg/kg for 4 weeks, significantly impedes the advancement of pulmonary hypertension and the formation of right ventricular hypertrophy. Additionally, when administered at a dosage of 1 mg/kg over 30 weeks, it markedly improves the survival rates of CHF rats, significantly reducing the hypertrophy of both ventricles and alleviating pulmonary congestion.
Chemical Properties
Molecular Weight491.52
FormulaC24H21N5O5S
Cas No.403604-85-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (254.31 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0345 mL10.1725 mL20.3451 mL101.7253 mL
5 mM0.4069 mL2.0345 mL4.0690 mL20.3451 mL
10 mM0.2035 mL1.0173 mL2.0345 mL10.1725 mL
20 mM0.1017 mL0.5086 mL1.0173 mL5.0863 mL
50 mM0.0407 mL0.2035 mL0.4069 mL2.0345 mL
100 mM0.0203 mL0.1017 mL0.2035 mL1.0173 mL

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