Edonentan
Based on 1 Customer Validation
Edonentan (BMS 207940) is an orally active, highly selective endothelin A receptor (ETA receptor) antagonist with a Ki value of 0.01 nM against human targets. Edonentan blocks the pressor response induced by Big Endothelin-1 in conscious normotensive rats and the pressor response induced by ET-1 in conscious normotensive cynomolgus monkeys. Edonentan can be used in research related to cardiovascular diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.13%
- No. CAS: 210891-04-6
- Fòrmula: C28H32N4O5S
- Peso molecular:536.64
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
ETA 10 pM (Ki) |
ETB 810 nM (Ki) |
In Vitro
Edonentan (Compound 16a) is a highly potent and selective ETA receptor antagonist, with a Ki value of 0.01 nM for human ETA receptors stably expressed in CHO cells, and exhibits a selectivity of up to 80,000-fold over human ETB receptors stably expressed in CHO cells[1].
Edonentan inhibits ET-1 (HY-P0202)-induced contraction of rabbit carotid artery rings, with a Kb value of 1.0 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Parmacokinetics
| Species | Dose | Route | AUC0-∞ | CL | Vss | T1/2 | MRT | Tmax | Cmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 μmol/Kg | i.v. | / | 5.4 mL/min/kg | 1.1 L/kg | 3.4 h | / | / | / | / |
| Rat[1] | 20 μmol/Kg | p.o. | / | / | / | / | / | 0.4 h | 28 μM | 100 % |
| Monkey[1] | 25 μmol/Kg | i.v. | 161 μM·h | 2.7 mL/min/kg | 0.25 L/kg | 14 h | 1.6 h | / | / | / |
| Monkey[1] | 25 μmol/Kg | p.o. | 41.5 μM·h | / | / | 17 h | / | 1.2 h | 16.1 μM | 26 % |
In Vivo
Edonentan (10 µM/kg; p.o.) exerts maximal inhibitory effects on ET-1-induced pressor responses in conscious normotensive cynomolgus monkeys[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:0.004 µM/kg (i.v.); 0.13 µM/kg (p.o.); 3 µM/kg (p.o.)
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Administration:i.v.; p.o.
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Result:Blocked big ET-1-induced pressor responses with an ED25 of 0.004 µM/kg intravenously and 0.13 µM/kg orally.
Inhibited the pressor response by 60-70% for at least 195 minutes at an oral dose of 3 µM/kg.
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Animal Model:(male) Cynomolgus Monkey[1]
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Dosage:10 µM/kg
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Administration:p.o.
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Result:Produced maximal inhibition of the ET-1 pressor response (40% at 15 minutes post-treatment).
Maintained significant inhibition still present 5 hours after dosing.
Chemical Information
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No. CAS 210891-04-6
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Appearance Solid
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Peso molecular 536.64
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Fòrmula C28H32N4O5S
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Color White to light yellow
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SMILES
CC(C)(C)CC(N(CC1=CC(C2=NC=CO2)=CC=C1C3=CC=CC=C3S(=O)(NC4=NOC(C)=C4C)=O)C)=O
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Synonyms
BMS 207940
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 55 mg/mL (102.49 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Murugesan N, et al. Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist. Journal of medicinal chemistry. 2003 Jan 02;46(1):125-37. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8634 mL | 9.3172 mL | 18.6345 mL | 46.5862 mL |
| 5 mM | 0.3727 mL | 1.8634 mL | 3.7269 mL | 9.3172 mL | |
| 10 mM | 0.1863 mL | 0.9317 mL | 1.8634 mL | 4.6586 mL | |
| 15 mM | 0.1242 mL | 0.6211 mL | 1.2423 mL | 3.1057 mL | |
| 20 mM | 0.0932 mL | 0.4659 mL | 0.9317 mL | 2.3293 mL | |
| 25 mM | 0.0745 mL | 0.3727 mL | 0.7454 mL | 1.8634 mL | |
| 30 mM | 0.0621 mL | 0.3106 mL | 0.6211 mL | 1.5529 mL | |
| 40 mM | 0.0466 mL | 0.2329 mL | 0.4659 mL | 1.1647 mL | |
| 50 mM | 0.0373 mL | 0.1863 mL | 0.3727 mL | 0.9317 mL | |
| 60 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7764 mL | |
| 80 mM | 0.0233 mL | 0.1165 mL | 0.2329 mL | 0.5823 mL | |
| 100 mM | 0.0186 mL | 0.0932 mL | 0.1863 mL | 0.4659 mL |
Edonentan Related Classifications
HY-15402 Related Classifications
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Keywords
- Edonentan
- 210891-04-6
- BMS 207940
- BMS207940
- BMS-207940
- Endothelin Receptor
- CHO cells
- conscious normotensive cynomolgus monkeys
- conscious normotensive rats
- endothelin-1 (ET-1)
- big endothelin-1 (big ET-1)
- human ETB receptors
- rabbit carotid artery rings
- endothelin A (ET?) receptor
- rat gastrointestinal homogenate
- Inhibitor
- inhibitor
- inhibit