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.
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- CAS No.: 264609-13-4
- 화학식: C28H34N4O6S
- 분자량:554.66
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보관:
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
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
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ETA 10 pM (Ki) |
ETB 810 nM (Ki) |
In Vitro
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.
In Vivo
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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CAS No. 264609-13-4
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분자량 554.66
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화학식 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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Synonyms
BMS 207940 hydrate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Edonentan hydrate Related Classifications
HY-15402D Related Classifications
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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