| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Nebentan has concentration-dependent inhibitory effects on the specific binding of [125I]endothelin-1 to endothelin ETA and ETB receptors, with Ki values for human and rat endothelin ETA receptors of 0.697 nM and 1.53 nM, respectively. With Ki values of 569 nM and 155 nM, respectively, for human and rat endothelin ETB receptors, YM598 has a lower affinity [1]. Nebentan concentration-dependently reduced the 10 nM endothelin-1-induced increase in [Ca2+]i in CHO cells and A10 cells when measuring intracellular Ca2+ concentration; the IC50 values were 26.2 nM in CHO cells and 26.7 nM in A10 cells, respectively [1].
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| ln Vivo |
Right ventricular hypertrophy and the development of pulmonary hypertension are markedly inhibited by nebentan (oral; 0.1–1 mg/kg; 4 weeks) [2]. Oral nebentan (1 mg/kg; 30 weeks) dramatically lowers pulmonary congestion and biventricular hypertrophy while also improving the poor survival rate of CHF rats [2].
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| References |
[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: |
| Molecular Formula |
C24H21N5O5S
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|---|---|
| Molecular Weight |
491.5190
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| CAS # |
403604-85-3
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| Related CAS # |
Nebentan potassium;342005-82-7
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
S(/C(/[H])=C(\[H])/C1C([H])=C([H])C([H])=C([H])C=1[H])(N([H])C1=C(C(=NC(C2N=C([H])C([H])=C([H])N=2)=N1)OC([H])([H])[H])OC1=C([H])C([H])=C([H])C([H])=C1OC([H])([H])[H])(=O)=O
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~254.31 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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