Edonentan hydrate
Edonentan hydrate (BMS 207940 hydrate) is an orally active, highly selective endothelin A receptor (ETA receptor) antagonist with a Ki value of 0.01 nM against human targets. Edonentan hydrate 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 hydrate can be used in research related to cardiovascular diseases.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 264609-13-4
- 分子式: C28H34N4O6S
- 分子量:554.66
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
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ETA 10 pM (Ki) |
ETB 810 nM (Ki) |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 264609-13-4
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分子量 554.66
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分子式 C28H34N4O6S
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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.O
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別名
BMS 207940 hydrate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Edonentan hydrate 関連分類
HY-15402D 関連分類
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Keywords
- Edonentan
- 264609-13-4
- 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