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Nebentan potassium

Catalog No. T36008 CAS 342005-82-7

Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan potassium 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 potassium, CAS 342005-82-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 84.00
2 mg	In stock	$ 123.00
5 mg	In stock	$ 198.00
10 mg	In stock	$ 328.00
25 mg	In stock	$ 579.00
50 mg	In stock	$ 928.00
100 mg	In stock	$ 1,260.00
500 mg	In stock	$ 2,530.00
1 mL * 10 mM (in DMSO)	In stock	$ 238.00

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Purity: 98.92%

Biological Description

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Storage & Solubility Information

Description	Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan potassium 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:0.679 nM (Ki)
In vitro	Nebentan potassium 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 potassium 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 potassium, when administered orally at a dosage of 0.1-1 mg/kg for 4 weeks, significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy. Furthermore, at a dosage of 1 mg/kg over 30 weeks, it considerably improves the survival rate of CHF rats, markedly reducing the hypertrophy of both ventricles and alleviating pulmonary congestion.

Molecular Weight	530.62
Formula	C24H21KN5O5S
CAS No.	342005-82-7

Storage

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

Solubility Information

DMSO: 125 mg/mL (236.02 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 potassium 342005-82-7 inhibitor inhibit

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