Molecular Formula | C23H20FNO5 |
Molar Mass | 409.41 |
Density | 1.357±0.06 g/cm3(Predicted) |
Melting Point | 171-172°C |
Boling Point | 639.1±55.0 °C(Predicted) |
Solubility | DMSO: soluble20mg/mL, clear |
Appearance | powder |
Color | white to beige |
pKa | 3.25±0.20(Predicted) |
Storage Condition | room temp |
In vitro study | PF-04418948 antagonizing the effects of butaprost and PGE2 on EFS-induced human myometrial contraction also antagonized pge2-induced mouse tracheal Carbachol presystolic ring relaxation. PF-04418948 completely inhibited mouse and guinea pig tracheal relaxation induced by ONO-AE1-259 and PGE2, respectively. From neutrophils isolated from BMT mice or HSCT parents, PF-04418948 recovered the formation of neutrophil extracellular NETs. |
In vivo study | In rats, PF-04418948(10 mg/kg, p.o.) reduced the mean peak skin blood flow response and AUC 0-60 by 41% and 61%, respectively. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.443 ml | 12.213 ml | 24.426 ml |
5 mM | 0.489 ml | 2.443 ml | 4.885 ml |
10 mM | 0.244 ml | 1.221 ml | 2.443 ml |
5 mM | 0.049 ml | 0.244 ml | 0.489 ml |
use | PF-04418948 is an orally effective, effective and selective prostaglandin EP2 receptor antagonist with IC50 of 16 nM. |
biological activity | PF-04418948 is an effective selective prostaglandin EP receptor antagonist with IC50 of 16 nM. Phase 1. |
target | TargetValue EP receptor () 16 nM |
Target | Value |
EP₂ receptor () | 16 nM |
in vitro study | PF-04418948 antagonize the effects of butaprost and PGE2 on EFS-induced contraction of human myometrium, and also antagonize PGE2-induced relaxation of carbachol preconstriction ring in mouse trachea. PF-04418948 completely inhibited tracheal relaxation in mice and guinea pigs caused by ONO-AE1-259 and PGE2, respectively. From BMT mice or isolated neutrophils from HSCT parents, the formation of neutrophil extracellular bacterial networks (NETs) was PF-04418948 restored. |
in vivo study | in rats, PF-04418948(10 mg/kg, p.o.) reduced the average skin blood flow peak response and AUC 0-60 by 41% and 61%, respectively. |