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Nebentan

Catalog No. T36007 CAS 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].

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Nebentan, CAS 403604-85-3

Pack Size	Availability	Price/USD
5 mg	Inquiry	$ 197.00
10 mg	Inquiry	$ 332.00
25 mg	Inquiry	$ 581.00
1 mL * 10 mM (in DMSO)	Inquiry	$ 224.00

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Biological Description

Chemical Properties

Storage & Solubility Information

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,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].
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.

Molecular Weight	491.52
Formula	C24H21N5O5S
CAS No.	403604-85-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (254.31 mM)

References and Literature

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.

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Keywords

Nebentan 403604-85-3 inhibitor inhibit

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