Zamicastat

SKU: orb1308925

Description

Zamicastat is a dopamine β-hydroxylase (DBH) inhibitor that also acts as a dual inhibitor of the efflux transporters P-gp and BCRP. This small molecule is used in research to study catecholamine regulation and transporter interactions in both cellular and animal models of cardiovascular and neurological diseases.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1080028-80-3
• MW: 401.47
• Purity: 99.58% (May vary between batches)
• Formula: C₂₁H₂₁F₂N₃OS
• SMILES: Fc1cc(F)c2OC[C@@H](Cc2c1)n1c(CCNCc2ccccc2)c[nH]c1=S
• Target: BCRP,P-gp,Hydroxylase
• Solubility: DMSO:150 mg/mL (373.63 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.96 mM)

Bioactivity

• Target IC50:
  BCRP:17.0 μM |Dopamine β-hydroxylase:|P-gp:73.8 μM
• In Vivo:
  In the Dahl SS rat, Zamicastat (10, 30 and 100 mg/kg/day; oral bolus, 7 days) is tested acutely against salt-induced hypertension. Zamicastat produces a dose-dependent decrease in blood pressure.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Zamicastat, P-gp, P-gp (P-glycoprotein), Pgp, P-glycoprotein, Cluster of differentiation 243, CD243, Breast cancer resistance protein, Dopamine beta-monooxygenase, Dopamine beta-hydroxylase, Dopamine β-hydroxylase, Dopamine β-monooxygenase, ABCB1, ABCG2, BIA 5-1058, BCRP, Inhibitor, Multidrug resistance protein 1, inhibit, MDR1

Compound Identifiers

PubChem CID

25052630