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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
|
ETA 10 pM (Ki) |
ETB 810 nM (Ki) |
Edonentan hydrate (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 hydrate 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.
Edonentan (10 µM/kg; p.o.) hydrate 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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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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- 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