Etamicastat
Etamicastat (BIA 5-453) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.
At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Etamicastat hydrochloride) usually boasts enhanced water solubility and stability.
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- CAS. Nr.: 760173-05-5
- Formel: C14H15F2N3OS
- Molecular Weight:311.35
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Speicherung:
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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Other In-stock Forms of Etamicastat
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 107 nM (DBH)[1]
In Vitro
Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Etamicastat (50 mg/kg; a single oral administration) exhibits moderate oral bioavailability (64%), Cmax (4.9 nM), and terminal elimination half-lives (T1/2=3.7 h) in male Wistar rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRi mice[1]
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Dosage:100 mg/kg
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Administration:Administered intraperitoneally
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Result:Led to a significant reduction of noradrenaline levels (36% control) in heart with concomitant increasing in dopamine levels (850% of control).
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Animal Model:Male Wistar rats[1]
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Dosage:50 mg/kg (Pharmacokinetic Analysis)
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Administration:Orally administered with at a dose volume of 10 mL/kg
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Result:Oral bioavailability (64%), Cmax (4.9 nM), and (T1/2=3.7 h).
Chemical Information
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CAS. Nr. 760173-05-5
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Molecular Weight 311.35
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Formel C14H15F2N3OS
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SMILES
S=C1NC=C(CCN)N1[C@H]2COC3=C(C=C(F)C=C3F)C2
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Synonyms
BIA 5-453
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Etamicastat Related Classifications
HY-14838 Related Classifications
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