Formulation: A solid
Formal Name: N-[2-[(2E)-6,7-dihydro-9,10-dimethoxy-4-oxo-2-[(2,4,6-trimethylphenyl)imino]-2H-pyrimido[6,1-a]isoquinolin-3(4H)-yl]ethyl]-urea
Purity: ≥95%
Formula Markup: C26H31N5O4
Formula Weight: 477,6
Shelf life (days): 1460
CAS Number: 1884461-72-6
Notes: Ensifentrine is a phosphodiesterase 3 (PDE3) inhibitor (IC50 = 0.4 nM).{51365} It is selective for PDE3 over PDE4 (IC50 = 1,479 nM). Ensifentrine reduces phytohemagglutinin-induced proliferation of isolated human monocytes in a concentration-dependent manner and inhibits LPS-induced increases of TNF-α protein levels in isolated human monocytes (IC50 = 520 nM). It increases cAMP levels in isolated human neutrophils when used at a concentration of 10 µM. Ensifentrine inhibits electric field stimulation-induced contractile responses in isolated guinea pig trachea in a concentration-dependent manner. Intranasal administration of ensifentrine (25% w/w) inhibits histamine-induced bronchoconstriction and tracheal edema in guinea pigs.
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