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Submit ReviewPF 04418948 is a potent prostaglandin E receptor 2 antagonist (PTGER2; EP2; IC50 = 16 nM for human EP2 receptors), which displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors and exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. PF 04418948 inhibits PGE2-induced increases in intracellular cAMP in vitro and reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).
Sold for research purposes under agreement from Pfizer Inc.
The Chemical Probes pages of the Structural Genomics Consortium website are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 04418948 is reviewed.
PF 04418948 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 409.41 |
公式 | C23H20FNO5 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1078166-57-0 |
PubChem ID | 25114442 |
InChI Key | LWJGMYMNSNVCEM-UHFFFAOYSA-N |
Smiles | FC(C=C4)=CC=C4C(N(C3)CC3(C(O)=O)COC2=CC1=CC=C(OC)C=C1C=C2)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 40.94 | 100 |
以下数据基于产品分子量 409.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.44 mL | 12.21 mL | 24.43 mL |
5 mM | 0.49 mL | 2.44 mL | 4.89 mL |
10 mM | 0.24 mL | 1.22 mL | 2.44 mL |
50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
参考文献是支持产品生物活性的出版物。
Birrell et al (2013) Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor. Br.J.Pharmacol. 168 129 PMID: 22747912
af Forselles et al (2011) In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist. Br.J.Pharmacol. 164 1847 PMID: 21595651
If you know of a relevant reference for PF 04418948, please let us know.
关键词: PF 04418948, PF 04418948 supplier, PF04418948, prostanoid, receptors, EP2, antagonists, potent, selective, PGE2, prostaglandins, PTGER2, Prostanoid, Receptors, 4818, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PF 04418948 的部分引用包括:
Wang et al (2015) Phosphorylation of STAT3 mediates the induction of cyclooxygenase-2 by cortisol in the human amnion at parturition. Sci Signal 8 PMID: 26508788
Liu et al (2016) Inhibition of lysyl oxidase by prostaglandin E2 via EP2/EP4 receptors in human amnion fibroblasts: Implications for parturition. Mol Cell Endocrinol 424 118 PMID: 26826430
Liu et al (2016) Oxidized phospholipid OxPAPC activates TRPA1 and contributes to chronic inflammatory pain in mice PLoS One 11 e0165200 PMID: 27812120
Perkins et al (2018) Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol. 19 1309 PMID: 30397349
Guillem-Llobat et al (2016) Aspirin prevents colorectal cancer metastasis in mice by splitting the crosstalk between platelets and tumor cells. Oncotarget 7 32462 PMID: 27074574
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