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.
For research use only. We do not sell to patients.
- CAS No.: 760173-05-5
- Formula: C14H15F2N3OS
- Molecular Weight:311.35
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Storage:
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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Molecular Weight 311.35
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Etamicastat Related Classifications
HY-14838 Related Classifications
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