PF 04418948
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PF-04418948 is an orally active, potent and selective prostaglandin EP2 receptor antagonist with an IC50 of 16 nM.
Prostaglandin E2 (PGE2) induces distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. It is far less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in both cells and tissues.
In vitro, PF-04418948 inhibited prostaglandin E2 (PGE2)-induced growth in cAMP with a functional KB value of 1.8 nM in cells expressing EP2 receptors.
In vivo, in the case of human myometrium, PF-04418948 caused a parallel, rightward shift of the butaprost-induced inhibition of the contractions that was induced by electrical field stimulation with an apparent KB of 5.4 nM. In dog bronchiole and mouse trachea, it produced the same shifts of the PGE2-induced relaxation curve with a KB of 2.5 nM and an apparent KB of 1.3 nM respectively. Moreover, in the mouse trachea, reversal of the PGE2-induced relaxation by PF-04418948 produced an IC50 value of 2.7 nM.In rats, PF-04418948 significantly weakens the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally. It was selective for EP2 receptors over homologous and unrelated receptors, enzymes and channels.
References:
1: af Forselles KJ, Root J, Clarke T, Davey D, Aughton K, Dack K, Pullen N. 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):1847-56. doi: 10.1111/j.1476-5381.2011.01495.x. Erratum in: Br J Pharmacol. 2012 Jun;166(3):1192. Dosage error in article text. PubMed PMID: 21595651; PubMed Central PMCID: PMC3246710.
2. Birrell MA, Maher SA, Buckley J, Dale N, Bonvini S, Raemdonck K, Pullen N, Giembycz MA, Belvisi MG. 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. 2013 Jan;168(1):129-38. doi: 10.1111/j.1476-5381.2012.02088.x. PubMed PMID: 22747912; PubMed Central PMCID: PMC3570009.
3. Säfholm J, Dahlén SE, Delin I, Maxey K, Stark K, Cardell LO, Adner M. PGE2 maintains the tone of the guinea pig trachea through a balance between activation of contractile EP1 receptors and relaxant EP2 receptors. Br J Pharmacol. 2013 Feb;168(4):794-806. doi: 10.1111/j.1476-5381.2012.02189.x. PubMed PMID: 22934927; PubMed Central PMCID: PMC3631371
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 409.41 |
Cas No. | 1078166-57-0 |
Formula | C23H20FNO5 |
Solubility | insoluble in EtOH; insoluble in H2O; insoluble in DMSO |
Chemical Name | 1-(4-fluorobenzoyl)-3-(((6-methoxynaphthalen-2-yl)oxy)methyl)azetidine-3-carboxylic acid |
SDF | Download SDF |
Canonical SMILES | FC1=CC=C(C=C1)C(N2CC(COC3=CC=C4C(C=CC(OC)=C4)=C3)(C(O)=O)C2)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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