Etamicastat


Catalog No. Size PriceQuantity
M18565-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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.

Product information

CAS Number: 760173-05-5

Molecular Weight: 311.35

Formula: C14H15F2N3OS

Chemical Name: 5-(2-aminoethyl)-1-[(3R)-6,8-difluoro-3,4-dihydro-2H-1-benzopyran-3-yl]-2,3-dihydro-1H-imidazole-2-thione

Smiles: NCCC1=CNC(=S)N1[C@@H]1CC2C=C(F)C=C(F)C=2OC1

InChiKey: CWWWTTYMUOYSQA-LLVKDONJSA-N

InChi: InChI=1S/C14H15F2N3OS/c15-9-3-8-4-11(7-20-13(8)12(16)5-9)19-10(1-2-17)6-18-14(19)21/h3,5-6,11H,1-2,4,7,17H2,(H,18,21)/t11-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM).

In Vivo:

Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels. 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.

Products are for research use only. Not for human use.

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