PF 04418948
- CAS No.
- 1078166-57-0
- Chemical Name:
- PF 04418948
- Synonyms
- CS-2852;PF-0441848;PF 04418948;PF-04418948 ，S7211;PF 04418948 USP/EP/BP;PF04418948; PF 04418948;PF-04418948 >=98% (HPLC);PF-04418948, 10 mM in DMSO;PF-04418948;PF04418948;PF 04418948;1-(4-Fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl...
- CBNumber:
- CB32701162
- Molecular Formula:
- C23H20FNO5
- Molecular Weight:
- 409.41
- MDL Number:
- MFCD24387541
- MOL File:
- 1078166-57-0.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Melting point | 171-172°C |
|---|---|
| Boiling point | 639.1±55.0 °C(Predicted) |
| Density | 1.357±0.06 g/cm3(Predicted) |
| storage temp. | room temp |
| solubility | DMSO: soluble20mg/mL, clear |
| form | powder |
| pka | 3.25±0.20(Predicted) |
| color | white to beige |
| InChI | InChI=1S/C23H20FNO5/c1-29-19-8-4-17-11-20(9-5-16(17)10-19)30-14-23(22(27)28)12-25(13-23)21(26)15-2-6-18(24)7-3-15/h2-11H,12-14H2,1H3,(H,27,28) |
| InChIKey | POJZIZBONPAWIV-UHFFFAOYSA-N |
| SMILES | N1(C(=O)C2=CC=C(F)C=C2)CC(COC2=CC=C3C(=C2)C=CC(OC)=C3)(C(O)=O)C1 |
| FDA UNII | I7Z38E70VF |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
| WGK Germany | 3 |
| Storage Class | 11 - Combustible Solids |
PF 04418948 price More Price(50)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | PZ0213 | PF-04418948 ≥98% (HPLC) | 1078166-57-0 | 25mg | $528 | 2026-04-30 | Buy |
| Sigma-Aldrich | PZ0213 | PF-04418948 ≥98% (HPLC) | 1078166-57-0 | 5mg | $118 | 2024-03-01 | Buy |
| Cayman Chemical | 15016 | PF-04418948 ≥98% | 1078166-57-0 | 5mg | $108 | 2026-04-30 | Buy |
| Cayman Chemical | 15016 | PF-04418948 ≥98% | 1078166-57-0 | 10mg | $161 | 2026-04-30 | Buy |
| Cayman Chemical | 15016 | PF-04418948 ≥98% | 1078166-57-0 | 50mg | $748 | 2026-04-30 | Buy |
PF 04418948 Chemical Properties, Uses, Production
Chemical Properties
White Solid
Uses
PF 04418948 acts as a novel, potent and selective prostoglandin EP2 receptor antagonist.
Uses
PF-04418948 has been used in TG (trigeminal ganglion) explant culture.
Biological Activity
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.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
Biochem/physiol Actions
PF-04418948 is a PGE2 Receptor (EP2) specific antagonist (IC50 = 16 nM) with greater than 2000-fold selectivity over other EP subtypes. PF-04418948 inhibits EP2 activity in smooth muscle preps from human, dog and mouse.
Synthesis
![3-Azetidinecarboxylic acid, 1-(4-fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-, ethyl ester](/CAS/20210305/GIF/1078166-69-4.gif)
1078166-69-4
1078166-57-0
Example 14b: Synthesis of 1-(4-fluorobenzoyl)-3-(((6-methoxynaphthalen-2-yl)oxy)methyl)azetidine-3-carboxylic acid 1-(4-Fluorobenzoyl)-3-(((6-methoxy-2-naphthalenyl)oxy)methyl)azetidine-3-carboxylic acid ester (50.0 g, 111.4 mmol, Preparation 33) was suspended in acetonitrile (500 mL), followed by addition of sodium trimethylsilanolate (14.1 g, 126 mmol) and water (2.05 mL, 114 mmol). The suspension was stirred at room temperature for 4 hours. Then, 10% (v/v) aqueous phosphoric acid (100 mL, 171 mmol) was added and the reaction mixture was continued to be stirred at room temperature for 1 h, followed by stirring at 0 °C for 2 h. The reaction mixture was then stirred for 2 h at room temperature. The precipitate was collected, washed twice with water (2 x 250 mL) and dried under reduced pressure to afford the target compound 1-(4-fluorobenzoyl)-3-(((6-methoxynaphthalen-2-yl)oxy)methyl)azetidine-3-carboxylic acid as a white solid in 85% yield (39.5 g). 1H NMR (400 MHz, CD3OD) δ: 3.84 (s, 3H), 4.27 (d, 1H), 4.42 (m, 2H), 4.44 (s, 2H), 4.67 (d, 1H), 7.07 (m, 2H), 7.20 (m, 4H), 7.63 (m, 2H), 7.72 (m, 2H); ES m/z 410 [M + H]+.
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.
storage
Store at -20°C
References
[1] Patent: US2008/280877, 2008, A1. Location in patent: Page/Page column 22
[2] Patent: US2008/280877, 2008, A1. Location in patent: Page/Page column 21-22
PF 04418948 Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Xuerong Chemical Technology Co., LTD | 18201727566 | 230497258@qq.com | China | 514 | 58 |
| Chemsky（shanghai）International Co.,Ltd. | 021-50135380 | shchemsky@sina.com | China | 32273 | 50 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7545 | 61 |
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4853 | 58 |
| Shanghai Synmedia Chemical Co., Ltd. | 021-38681880 13817889927 | sales@synmedia-chem.com | China | 249 | 58 |
| Bide Pharmatech Ltd. | 400-164-7117 18317119277 | product02@bidepharm.com | China | 40000 | 60 |
| Mashilabs (Shanghai) Co.,Ltd. | 19916721580 | mafarm@126.com | China | 4534 | 58 |
| AdooQ Bioscience CHINA | 025-58849295 | info@adooq.cn | China | 2981 | 60 |
| Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51389 | 80 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4859 | 55 |
View Latest Price from PF 04418948 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2026-07-14 | PF-04418948
1078166-57-0
|
$40.00-90.00 | 98.67% | 10g | TargetMol Chemicals Inc. | ||
 |
2019-12-26 | PF 04418948
1078166-57-0
|
$1.00 | 1KG | 97%-99.9% | 100kg | Career Henan Chemical Co |
-
- PF-04418948
1078166-57-0
- $40.00-90.00
- 98.67%
- TargetMol Chemicals Inc.
-
- PF 04418948
1078166-57-0
- $1.00
- 97%-99.9%
- Career Henan Chemical Co
