Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ensifentrine (Ensifentrinum) is a PDE3/4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 41.00 | |
5 mg | In stock | $ 97.00 | |
10 mg | In stock | $ 163.00 | |
25 mg | In stock | $ 347.00 | |
50 mg | In stock | $ 563.00 | |
100 mg | In stock | $ 913.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 107.00 |
Description | Ensifentrine (Ensifentrinum) is a PDE3/4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis. |
Targets&IC50 | PDE3:0.4 nM, PDE4:1479 nM |
In vitro | Electrical field stimulation-induced contraction of guinea pig superfused isolated tracheal preparations was significantly inhibited by Ensifentrine (10 microM) (percentage control; 93 +/- 1.2). Contractile responses were suppressed for up to 12 h after termination of superfusion with Ensifentrine demonstrating a long duration of action. Ensifentrine4 inhibited, in a concentration-dependent manner, lipopolysaccharide-induced tumor necrosis factor alpha release from human monocytes [IC50; 0.52 microM (0.38-0.69)] and proliferation of human mononuclear cells to phytohemagglutinin [IC50; 0.46 microM (0.24-0.9)][2]. |
In vivo | Ensifentrine administered orally significantly inhibited eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs. Likewise, inhalation of dry powder containing Ensifentrine by conscious guinea pigs (25% in micronized lactose) 1.5 h before antigen exposure significantly inhibited the recruitment of eosinophils to the airways. Exposure of conscious guinea pigs to inhalation of dry powder containing Ensifentrine (2.5%) and RPL565 (25%) in micronized lactose significantly inhibited histamine-induced plasma protein extravasation in the trachea and histamine-induced bronchoconstriction over a 5.5-h period[2]. |
Synonyms | Ensifentrina, Ensifentrinum |
Molecular Weight | 477.56 |
Formula | C26H31N5O4 |
CAS No. | 1884461-72-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/ml(41.88 mM)
You can also refer to dose conversion for different animals. More
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Ensifentrine 1884461-72-6 Metabolism PDE RPL 554 RPL554 inhaled Inhibitor RPL-554 bronchoprotective inhibit COPD PDE4 Ensifentrina anti-inflammatory Ensifentrinum PDE3 Phosphodiesterase (PDE) inhibitor