| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
ETA 0.679 nM (Ki) ETB 569 nM (Ki)
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|---|---|
| ln Vitro |
In a concentration-dependent manner, nebentan potassium blocks the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors; the Ki values for human and rat endothelin ETA receptors are 0.697 nM and 1.53 nM, respectively. By comparison, YM598 has low affinities, with Ki values of 569 nM and 155 nM for rat and human endothelin ETB receptors, respectively[1]. Nebentan potassium concentration-dependently suppresses the increase in [Ca2+]i induced by 10 nM endothelin-1 in both CHO and A10 cells when measuring intracellular Ca2+ concentration; the IC50 values for CHO cells are 26.2 nM and 26.7 nM, respectively[1].
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| ln Vivo |
When taken orally for four weeks at a dose of 0.1–1 mg/kg, nebentan potassium dramatically slows the advancement of pulmonary hypertension and right ventricular hypertrophy[2]. Nebentan potassium (oral; 1 mg/kg; 30 weeks) considerably lowers both pulmonary congestion and both ventricle hypertrophy, which in turn improves 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 |
C24H20KN5O5S
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|---|---|
| Molecular Weight |
529.61
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| CAS # |
342005-82-7
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| Related CAS # |
Nebentan;403604-85-3
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| SMILES |
COC1N=C(C2N=CC=CN=2)N=C([N-]S(/C=C/C2C=CC=CC=2)(=O)=O)C=1OC1C=CC=CC=1OC.[K+]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (236.02 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.15 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 16.7 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: ≥ 1.67 mg/mL (3.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (3.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8882 mL | 9.4409 mL | 18.8818 mL | |
| 5 mM | 0.3776 mL | 1.8882 mL | 3.7764 mL | |
| 10 mM | 0.1888 mL | 0.9441 mL | 1.8882 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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