PF04418948
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522468

CAS#: 1078166-57-0

Description: PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist. PF-04418948 inhibited prostaglandin E(2)(PGE(2))-induced increase in cAMP in cells expressing EP(2) receptors with a functional K(B) value of 1.8 nM. In human myometrium, PF-04418948 produced a parallel, rightward shift of the butaprost-induced inhibition of the contractions induced by electrical field stimulation with an apparent K(B) of 5.4 nM. In dog bronchiole and mouse trachea, PF-04418948 produced parallel rightward shifts of the PGE(2)-induced relaxation curve with a K(B) of 2.5 nM and an apparent K(B) of 1.3 nM respectively. Reversal of the PGE(2)-induced relaxation in the mouse trachea by PF-04418948 produced an IC(50) value of 2.7 nM.


Chemical Structure

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PF04418948
CAS# 1078166-57-0

Theoretical Analysis

MedKoo Cat#: 522468
Name: PF04418948
CAS#: 1078166-57-0
Chemical Formula: C23H20FNO5
Exact Mass: 409.13255
Molecular Weight: 409.41
Elemental Analysis: C, 67.48; H, 4.92; F, 4.64; N, 3.42; O, 19.54

Size Price Shipping out time Quantity
10mg USD 110 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 750 Same day
200mg USD 1250 Same day
500mg USD 2250 Same day
1g USD 3250 2 Weeks
2g USD 5450 2 Weeks
5g USD 8950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-02-25. Prices are subject to change without notice.

PF04418948, purity > 98%, is in stock. The same day shipping out after order is received.

Synonym: PF04418948; PF-04418948; PF 04418948; PF4418948; PF-4418948; PF 4418948.

IUPAC/Chemical Name: 1-(4-Fluorobenzoyl)-3-[[(6-methoxy-2-naphthalenyl)oxy]methyl]-3-azetidinecarboxylic acid

InChi Key: LWJGMYMNSNVCEM-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(C1(COC2=CC=C3C=C(OC)C=CC3=C2)CN(C(C4=CC=C(C=C4)F)=O)C1)O

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Domingo-Gonzalez R, Martínez-Colón GJ, Smith AJ, Smith CK, Ballinger MN, Xia M, Murray S, Kaplan MJ, Yanik GA, Moore BB. Prostaglandin E(2) Inhibits Neutrophil Extracellular Trap Formation Post-stem Cell Transplant. Am J Respir Crit Care Med. 2015 Sep 29. [Epub ahead of print] PubMed PMID: 26417909.

2: Säfholm J, Manson ML, Bood J, Delin I, Orre AC, Bergman P, Al-Ameri M, Dahlén SE, Adner M. Prostaglandin E(2) inhibits mast cell-dependent bronchoconstriction in human small airways through the E prostanoid subtype 2 receptor. J Allergy Clin Immunol. 2015 May 9. pii: S0091-6749(15)00489-3. doi: 10.1016/j.jaci.2015.04.002. [Epub ahead of print] PubMed PMID: 25962903.

3: Martinez-Cutillas M, Mañé N, Gallego D, Jimenez M, Martin MT. EP2 and EP4 receptors mediate PGE2 induced relaxation in murine colonic circular muscle: pharmacological characterization. Pharmacol Res. 2014 Dec;90:76-86. doi: 10.1016/j.phrs.2014.10.001. Epub 2014 Oct 20. PubMed PMID: 25461458.

4: Jiao HY, Kim DH, Ki JS, Ryu KH, Choi S, Jun JY. Effects of lubiprostone on pacemaker activity of interstitial cells of cajal from the mouse colon. Korean J Physiol Pharmacol. 2014 Aug;18(4):341-6. doi: 10.4196/kjpp.2014.18.4.341. Epub 2014 Aug 13. PubMed PMID: 25177167; PubMed Central PMCID: PMC4146637.

5: Stone AJ, Copp SW, Kaufman MP. Role of prostaglandins in spinal transmission of the exercise pressor reflex in decerebrated rats. Neuroscience. 2014 Sep 26;277:26-35. doi: 10.1016/j.neuroscience.2014.06.061. Epub 2014 Jul 5. PubMed PMID: 25003710; PubMed Central PMCID: PMC4164591.

6: Shimizu T, Tanaka K, Nakamura K, Taniuchi K, Yawata T, Higashi Y, Ueba T, Dimitriadis F, Shimizu S, Yokotani K, Saito M. Possible involvement of brain prostaglandin E2 and prostanoid EP3 receptors in prostaglandin E2 glycerol ester-induced activation of central sympathetic outflow in the rat. Neuropharmacology. 2014 Jul;82:19-27. doi: 10.1016/j.neuropharm.2014.03.005. Epub 2014 Mar 19. PubMed PMID: 24657150.

7: Cheah EY, Burcham PC, Mann TS, Henry PJ. Acrolein relaxes mouse isolated tracheal smooth muscle via a TRPA1-dependent mechanism. Biochem Pharmacol. 2014 May 1;89(1):148-56. doi: 10.1016/j.bcp.2014.02.009. Epub 2014 Feb 19. PubMed PMID: 24561178.

8: Kach J, Sandbo N, La J, Denner D, Reed EB, Akimova O, Koltsova S, Orlov SN, Dulin NO. Antifibrotic effects of noscapine through activation of prostaglandin E2 receptors and protein kinase A. J Biol Chem. 2014 Mar 14;289(11):7505-13. doi: 10.1074/jbc.M113.546812. Epub 2014 Feb 3. PubMed PMID: 24492608; PubMed Central PMCID: PMC3953264.

9: Säfholm J, Dahlén SE, Adner M. Antagonising EP1 and EP2 receptors reveal that the TP receptor mediates a component of antigen-induced contraction of the guinea pig trachea. Eur J Pharmacol. 2013 Oct 15;718(1-3):277-82. doi: 10.1016/j.ejphar.2013.08.021. Epub 2013 Sep 5. PubMed PMID: 24012781.

10: Kay LJ, Gilbert M, Pullen N, Skerratt S, Farrington J, Seward EP, Peachell PT. Characterization of the EP receptor subtype that mediates the inhibitory effects of prostaglandin E2 on IgE-dependent secretion from human lung mast cells. Clin Exp Allergy. 2013 Jul;43(7):741-51. doi: 10.1111/cea.12142. PubMed PMID: 23786281.

11: 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.

12: 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.

13: 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.

14: Birrell MA, Nials AT. At last, a truly selective EP₂ receptor antagonist. Br J Pharmacol. 2011 Dec;164(7):1845-6. doi: 10.1111/j.1476-5381.2011.01494.x. PubMed PMID: 21595650; PubMed Central PMCID: PMC3246709.