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Nebentan

Name: Nebentan
Brand: TargetMol
SKU: T36007
Rating: 4.5 (1 reviews)

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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

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Catalog No. T36007Cas No. 403604-85-3

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$197	Inquiry	Inquiry
10 mg	$332	Inquiry	Inquiry
25 mg	$581	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$224	Inquiry	Inquiry

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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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	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, 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 Weight	491.52
Formula	C₂₄H₂₁N₅O₅S
Cas No.	403604-85-3
Smiles	COc1ccccc1Oc1c(NS(=O)(=O)\C=C\c2ccccc2)nc(nc1OC)-c1ncccn1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (254.31 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.71 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0345 mL	10.1725 mL	20.3451 mL	101.7253 mL
5 mM	0.4069 mL	2.0345 mL	4.0690 mL	20.3451 mL
10 mM	0.2035 mL	1.0173 mL	2.0345 mL	10.1725 mL
20 mM	0.1017 mL	0.5086 mL	1.0173 mL	5.0863 mL
50 mM	0.0407 mL	0.2035 mL	0.4069 mL	2.0345 mL
100 mM	0.0203 mL	0.1017 mL	0.2035 mL	1.0173 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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