| Description | PF-04418948 is a potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM). |
| Target activity | EP2 receptor:16 nM |
| Synonyms | PF 04418948, PF04418948 |
| molecular weight | 409.41 |
| Molecular formula | C23H20FNO5 |
| CAS | 1078166-57-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (109.91 mM), Sonication is recommended. |
| References | 1. af Forselles KJ, et al. In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist. Br J Pharmacol. 2011 Dec;164(7):1847-1856 2. Birrell MA, et al. Br J Pharmacol. 2013 Jan;168(1):129-38. 3. Lu W, Yu W, He J, et al. Reprogramming immunosuppressive myeloid cells facilitates immunotherapy for colorectal cancer[J]. EMBO Molecular Medicine. 2020: e12798. |
| Citations | 1. Lu W, Yu W, He J, et al. Reprogramming immunosuppressive myeloid cells facilitates immunotherapy for colorectal cancer. EMBO Molecular Medicine. 2020: e12798. |