PF 04418948是一种具有口服活性、强效且选择性的前列腺素EP2受体拮抗剂，IC50值为16nM。
Cas No.:1078166-57-0
Sample solution is provided at 25 µL, 10mM.
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PF 04418948 is an orally active, potent, and selective prostaglandin EP2 receptor antagonist with an IC50 value of 16nM [1]. PF 04418948 can inhibit the production of nitrite in microglia and reduce the accumulation of cyclic adenosine monophosphate (cAMP) by inhibiting the EP2 receptor[2]. PF 04418948 is widely used to inhibit the activation of satellite glial cells (SGCs) and alleviate the progression of temporomandibular joint osteoarthritis[3].
In vitro, PF 04418948 treatment (10nM) for 30 minutes significantly inhibited the excitatory effects of butaprost and treprostinil, and reduced the firing frequency of isolated rat locus coeruleus neurons[4]. Four days of treatment with 1µM PF 04418948 significantly inhibited the anti-proliferative effect of treprostinil on human pulmonary artery smooth muscle cells (hPASMCs) and prevented the activation of EP2 receptors[5]. 1µM of PF 04418948 pretreatment for 30 minutes significantly reduced the secretion of IL-6 by the growth-arrested human airway smooth muscle (ASM) cells, and inhibited the expression of IL-6 and COX-2 mRNA[6].
In vivo, PF 04418948 treatment via intraperitoneal injection at a dose of 10mg/kg/day for 10 days significantly alleviated the colitis induced by dextran sodium sulfate (DSS) in mice, and improved the weight loss and shortening of the colon in the mice[7]. Intracerebroventricular injection of PF 04418948 (5µl; 100nmol/rat) for 30 minutes significantly attenuated the changes in threshold pressure required to induce micturition (TP) induced by PGE2 (1nmol/rat)[8].
References:
[1] Af Forselles K J, Root J, Clarke T, et al. In vitro and in vivo characterization of PF‐04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist[J]. British journal of pharmacology, 2011, 164(7): 1847-1856.
[2] Nagano T, Nishiyama R, Sanada A, et al. Prostaglandin E2 potentiates interferon‐γ‐induced nitric oxide production in cultured rat microglia[J]. Journal of neurochemistry, 2017, 140(4): 605-612.
[3] Ma X, Yuan Y, Zhu T, et al. EP2 Modulates Satellite Glial Cell Activation in Temporomandibular Joint Osteoarthritis Chronic Pain via p-ERK1/2 Signaling[J]. Journal of dental research, 2025, 104(10): 1127-1137.
[4] Nazabal A, Mendiguren A, Pineda J. Pharmacological characterization of prostaglandin E2 EP2 and EP4 receptors in male rat locus coeruleus neurons ex vivo[J]. Biochemical Pharmacology, 2024, 230: 116602.
[5] Patel J A, Shen L, Hall S M, et al. Prostanoid EP2 receptors are up-regulated in human pulmonary arterial hypertension: a key anti-proliferative target for treprostinil in smooth muscle cells[J]. International journal of molecular sciences, 2018, 19(8): 2372.
[6] Bradbury P, Rumzhum N N, Ammit A J. EP2 and EP4 receptor antagonists: Impact on cytokine production and β2‐adrenergic receptor desensitization in human airway smooth muscle[J]. Journal of Cellular Physiology, 2019, 234(7): 11070-11077.
[7] Wang C, Yu T, Wang Y, et al. Targeting the EP2 receptor ameliorates inflammatory bowel disease in mice by enhancing the immunosuppressive activity of Treg cells[J]. Mucosal Immunology, 2025, 18(2): 418-430.
[8] Shimizu T, Shimizu N, Tsubouchi S, et al. Centrally administered prostaglandin E2 suppresses the micturition reflex in rats[J]. Journal of Pharmacological Sciences, 2025, 158(3): 231-237.
PF 04418948是一种具有口服活性、强效且选择性的前列腺素EP2受体拮抗剂，IC50值为16nM[1]。PF 04418948可通过抑制EP2受体，抑制小胶质细胞中亚硝酸盐的产生，并减少环磷酸腺苷（cAMP）的积累[2]。PF 04418948被广泛用于抑制卫星胶质细胞（SGCs）的活化，并缓解颞下颌关节骨关节炎的进展[3]。
在体外，使用10nM的PF 04418948处理分离的大鼠蓝斑神经元30分钟，显著抑制了butaprost和treprostinil的兴奋效应，并降低了神经元的放电频率[4]。使用1µM的PF 04418948处理 4 天，显著抑制了treprostinil对人肺动脉平滑肌细胞（hPASMCs）的抗增殖作用，并阻止了EP2受体的激活[5]。使用1µM的PF 04418948预处理生长停滞的人气道平滑肌（ASM）细胞30分钟，显著减少了IL-6的分泌，并抑制了IL-6和COX-2 mRNA的表达[6]。
在体内，每日腹腔注射10mg/kg剂量的PF 04418948，连续10天，显著减轻了葡聚糖硫酸钠（DSS）诱导的小鼠结肠炎，并改善了小鼠的体重下降和结肠缩短[7]。脑室内注射PF 04418948（5µl；100nmol/大鼠）30分钟，显著减弱了PGE2（1nmol/大鼠）引起的大鼠诱发排尿（TP）所需阈值压力的变化[8]。
| Cell experiment [1]: | |
Cell lines | Human airway smooth muscle (ASM) cells |
Preparation Method | Human ASM cells were cultured in DMEM medium supplemented with 10% fetal bovine serum (FBS), 5mg/ml of penicillin, and 5mg/ml of streptomycin at 37℃ in the presence of 5% CO2. Growth-arrested ASM cells were pretreated for 30min with a range of concentrations (0, 0.25, 0.5, 1, 2.5, 5, and 10µM) of PF 04418948 (EP2 receptor antagonist) or vehicle controls, before 24h treatment with PGE2 (100nM). IL-6 protein secretion was measured by ELISA. |
Reaction Conditions | 0, 0.25, 0.5, 1, 2.5, 5, and 10µM; 30min |
Applications | PF 04418948 treatment reduced the PGE2-induced IL-6 protein secretion in ASM cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Male C57BL/6J mice (6-weeks-old) were maintained in the specific pathogen-free animal laboratory in an environment with a controlled temperature (22±1°C) and relative humidity (50±5%) on a 12:12-h light/dark cycle, with free access to sterile food and water. For DSS-induced colitis, mice were subjected to DSS treatment (2% in drinking water) for 6-9 days. After 5 days of DSS treatment, mice were given daily doses of 10mg/kg PF 04418948 by intraperitoneal (i.p.) injections for an additional 10 days. Then, colon samples from the mice were collected for analysis. |
Dosage form | 10mg/kg/day for 10 days; i.p. |
Applications | PF 04418948 administration significantly improved DSS-induced weight loss and colon shortening in mice. |
References: | |
| Cas No. | 1078166-57-0 | SDF | |
| 化学名 | 1-(4-fluorobenzoyl)-3-(((6-methoxynaphthalen-2-yl)oxy)methyl)azetidine-3-carboxylic acid | ||
| Canonical SMILES | FC1=CC=C(C=C1)C(N2CC(COC3=CC=C4C(C=CC(OC)=C4)=C3)(C(O)=O)C2)=O | ||
| 分子式 | C23H20FNO5 | 分子量 | 409.41 |
| 溶解度 | <0.834mg/mL in EtOH, Limited solubility in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4425 mL | 12.2127 mL | 24.4254 mL |
| 5 mM | 488.5 μL | 2.4425 mL | 4.8851 mL |
| 10 mM | 244.3 μL | 1.2213 mL | 2.4425 mL |
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