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.
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- CAS No.: 760173-05-5
- Formule: C14H15F2N3OS
- Masse moléculaire:311.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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. Further protocols information, click here.
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 No. 760173-05-5
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Masse moléculaire 311.35
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Etamicastat Related Classifications
HY-14838 Related Classifications
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