A DβH inhibitor
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Zamicastat

Item No. 42101

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(3R)-6,8-difluoro-3,4-dihydro-2H-1-benzopyran-3-yl]-1,3-dihydro-5-[2-[(phenylmethyl)amino]ethyl]-2H-imidazole-2-thione
CAS Number
1080028-80-3
Synonyms
  • BIA 5-1058
Molecular Formula
C21H21F2N3OS
Formula Weight
401.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
S=C1NC=C(CCNCC2=CC=CC=C2)N1[C@H]3COC4=C(F)C=C(F)C=C4C3
InChi Code
InChI=1S/C21H21F2N3OS/c22-16-8-15-9-18(13-27-20(15)19(23)10-16)26-17(12-25-21(26)28)6-7-24-11-14-4-2-1-3-5-14/h1-5,8,10,12,18,24H,6-7,9,11,13H2,(H,25,28)/t18-/m1/s1
InChi Key
ZSSLCFLHEFXANG-GOSISDBHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $65

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    5 mg

    $195

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    10 mg

    $325

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    25 mg

    $650

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    Product Description

    Zamicastat is an inhibitor of dopamine β-hydroxylase (DβH).1 It increases levels of norepinephrine and decreases levels of dopamine in the hearts of aged spontaneously hypertensive rats (SHRs) when administered at a dose of 30 mg/kg per day. Zamicastat decreases diastolic and systolic blood pressure in the same model. It increases serum levels of erythropoietin (EPO), decreases the heart-to-body weight ratio, and increases survival in a mouse model of hypertension using aged rats fed a high-salt diet.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Igreja, B., Pires, N., Loureiro, A., et al. Cardiometabolic and inflammatory benefits of sympathetic down-regulation with zamicastat in aged spontaneously hypertensive rats. ACS Pharmacol. Transl. Sci. 2(5), 353-360 (2019).

    2. Igreja, B., Pires, N.M., Wright, L.C., et al. Effects of zamicastat treatment in a genetic model of salt-sensitive hypertension and heart failure. Eur. J. Pharmacol. 842, 125-132 (2019).