product name PF-04418948
Description: PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist. PF-04418948 inhibited prostaglandin E2(PGE2-induced increase in cAMP in cells expressing EP2 receptors with a functional KB value of 1.8 nM. In human myometrium, PF-04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractions induced by electrical field stimulation with an apparent KB of 5.4 nM. In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of the PGE2-induced relaxation curve with a KB of 2.5 nM and an apparent KB of 1.3 nM respectively. Reversal of the PGE2-induced relaxation in the mouse trachea by PF-04418948 produced an IC50 value of 2.7 nM.
References: Br J Pharmacol. 2011 Dec;164(7):1847-56; Br J Pharmacol. 2013 Jan;168(1):129-38.
409.41
Formula
C23H20FNO5
CAS No.
1078166-57-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 81 mg/mL (197.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: PF-04418948 antagonizes the effects of butaprost and PGE2 on an EFS-induced contraction of the human myometrium, and antagonizes PGE2-induced relaxation of carbachol pre-contracted rings of mouse trachea. PF-04418948 competitively inhibits relaxations of murine and guinea pig trachea induced by ONO-AE1-259 and PGE2 respectively. PF-04418948 restores neutrophil extracellular traps (NETs) formation in neutrophils isolated from BMT mice or HSCT patients. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In Rats, PF-04418948 (10 mg/kg, p.o.) reduces the mean cutaneous blood flow peak response and AUC0–60 by 41% and 61%, respectively. |
| Animal model | Sprague Dawley rats |
| Formulation & Dosage | Formulated in 0.5% w/v methylcellulose + 0.1% v/v Tween 80 in purified water; 10 mg/kg; p.o. |
| References | Br J Pharmacol. 2011 Dec;164(7):1847-56; Br J Pharmacol. 2013 Jan;168(1):129-38. |
