PF 04418948

Pricing Availability   Qty
说明: Potent and selective EP2 receptor antagonist
化学名: 1-(4-Fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-3-azetidinecarboxylic acid
纯度: ≥98% (HPLC)
说明书
引用文献 (5)
评论

生物活性 for PF 04418948

PF 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).

许可信息

Sold for research purposes under agreement from Pfizer Inc.

External Portal Information for PF 04418948

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.

化合物库 for PF 04418948

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。

技术数据 for PF 04418948

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.

溶解性数据 for PF 04418948

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 40.94 100

制备储备液 for PF 04418948

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.

选择批次从而根据批次分子量重新计算:
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

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产品说明书 for PF 04418948

分析证书/产品说明书
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参考文献 for PF 04418948

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.

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关键词: PF 04418948, PF 04418948 supplier, PF04418948, prostanoid, receptors, EP2, antagonists, potent, selective, PGE2, prostaglandins, PTGER2, Prostanoid, Receptors, 4818, Tocris Bioscience

5 篇 PF 04418948 的引用文献

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


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