Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC 50 s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research In Vitro Ensifentrine (RPL-554) inhibits, in a concentration-dependent manner, lipopolysaccharide-induced TNF-α release from human monocytes (IC 50 of 0.52 μM) and proliferation of human mononuclear cells to phytohemagglutinin (IC 50 of 0.46 μM). Electrical field stimulation-induced contraction of guinea pig superfused isolated tracheal preparations is significantly inhibited by Ensifentrine (10 μM). Contractile responses are suppressed for up to 12 h after termination of superfusion with RPL-554 demonstrating a long duration of action. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Ensifentrine (RPL-554; 10 mg/kg; Oral administration; once) significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs . The inhalation of dry powder containing Ensifentrine by conscious guinea pigs (25% in micronized lactose) 1.5 h before antigen exposure significantly inhibits the recruitment of eosinophils to the airways . Exposure of conscious guinea pigs to inhalation of dry powder containing Ensifentrine (2.5%) in micronized lactose significantly inhibits histamine-induced plasma protein extravasation in the trachea and histamine-induced bronchoconstriction over a 5.5-h period . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Dunkin Hartley guinea pigs (200-300 g) injected with ovalbumin . Dosage: 10 mg/kg Administration: Oral administration; once Result: Significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs. Form:Solid IC50& Target:PDE3 0.4 nM (IC 50 ) PDE4 1479 nM (IC 50 )
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Ensifentrine
CAS number：1884461-72-6 molecular formula：C26H31N5O4
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| Chinese alias | 恩替芬特林 | ||
| English alias | AKOS001475841 | EPA Pesticide Chemical Code 111902 | GTPL11865 | EX-A6633 | 4,6-dimethylisothiazolo[5,4-b]pyridin-3-ol | Urea, N-(2-(6,7-dihydro-9,10-dimethoxy-4-oxo-2-((2,4,6-trimethylphenyl)imino)-2H-pyrimido(6,1-a)isoquinolin-3(4H)-yl)ethyl)- | FT-0670 | ||
| CAS number | 1884461-72-6 | molecular formula | C26H31N5O4 |
| molecular weight | 477.56 g/mol | Exact mass | ≥99% |
| PSA | 109.000 Ų | logp | 2.700 |
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