1. GPCR/G Protein
  2. Endothelin Receptor
  3. Nebentan

Nebentan (Synonyms: YM598 free base)

Cat. No.: HY-106994 Purity: 99.67%
Handling Instructions

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. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.

For research use only. We do not sell to patients.

Nebentan Chemical Structure

Nebentan Chemical Structure

CAS No. : 403604-85-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 270 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 400 In-stock
Estimated Time of Arrival: December 31
25 mg USD 700 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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 (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].

IC50 & Target[1]

ETA

0.697 nM (Ki)

ETB

569 nM (Ki)

In Vitro

Nebentan inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dependent manner, Ki 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 ETB receptors, with Ki values of 569 nM and 155 nM,respectively[1].
In measurement of intracellular Ca2+ concentration, Nebentan concentration-dependently inhibits the increase in [Ca2+]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively[1].

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[2].
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[2].

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

Clinical Trial
Molecular Weight

491.52

Formula

C₂₄H₂₁N₅O₅S

CAS No.

403604-85-3

SMILES

O=S(/C=C/C1=CC=CC=C1)(NC2=NC(C3=NC=CC=N3)=NC(OC)=C2OC4=CC=CC=C4OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (254.31 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0345 mL 10.1725 mL 20.3451 mL
5 mM 0.4069 mL 2.0345 mL 4.0690 mL
10 mM 0.2035 mL 1.0173 mL 2.0345 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.23 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.23 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NebentanYM598YM 598YM-598Endothelin ReceptorA10endothelinCHOventricularhypertrophyCHFHeart Failurenon-peptidecor pulmonalemyocardial infarctionInhibitorinhibitorinhibit

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Nebentan
Cat. No.:
HY-106994
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