Ensifentrine
Modify Date: 2024-01-05 06:11:24
Ensifentrine structure
|
Common Name | Ensifentrine | ||
|---|---|---|---|---|
| CAS Number | 1884461-72-6 | Molecular Weight | 477.56 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H31N5O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of EnsifentrineEnsifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s 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[1][2]. |
| Name | Ensifentrine |
|---|
| Description | Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s 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[1][2]. |
|---|---|
| Related Catalog | |
| Target |
PDE3:0.4 nM (IC50) PDE4:1479 nM (IC50) |
| In Vitro | Ensifentrine (RPL-554) inhibits, in a concentration-dependent manner, lipopolysaccharide-induced TNF-α release from human monocytes (IC50 of 0.52 μM) and proliferation of human mononuclear cells to phytohemagglutinin (IC50 of 0.46 μM)[1]. 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[1]. |
| In Vivo | Ensifentrine (RPL-554; 10 mg/kg; Oral administration; once) significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs[1]. 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[1]. 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[1]. Animal Model: Male Dunkin Hartley guinea pigs (200-300 g) injected with ovalbumin[1]. Dosage: 10 mg/kg Administration: Oral administration; once Result: Significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs. |
| References |
| Molecular Formula | C26H31N5O4 |
|---|---|
| Molecular Weight | 477.56 |