Molecular structure of GW 848687X, CAS Number: 612831-24-0
GW 848687X (CAS 612831-24-0)
CAS Number:
612831-24-0
Molecular Weight:
441.9
Molecular Formula:
C24H18ClF2NO3
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GW 848687X, a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM), exhibits over 400-fold selectivity for EP1 in comparison to other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. Additionally, it demonstrates a 30-fold selectivity over the thromboxane A2 receptor, TP, and acts as a functional antagonist at higher concentrations. Its interactions with the FP and CRTH2/DP2 receptors remain uncharacterized. EP1 is a prostanoid receptor—which are a subtype of G protein-coupled receptors—that initiates cellular signaling upon interaction with PGE2.
GW 848687X (CAS 612831-24-0) References
- The discovery of 6-[2-(5-chloro-2-{[(2,4-difluorophenyl)methyl]oxy}phenyl)-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid, GW848687X, a potent and selective prostaglandin EP1 receptor antagonist for the treatment of inflammatory pain. | Giblin, GM., et al. 2007. Bioorg Med Chem Lett. 17: 385-9. PMID: 17084082
- Discovery of GSK345931A: An EP(1) receptor antagonist with efficacy in preclinical models of inflammatory pain. | Hall, A., et al. 2009. Bioorg Med Chem Lett. 19: 497-501. PMID: 19036582
- Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain. | Hall, A., et al. 2009. Bioorg Med Chem Lett. 19: 2599-603. PMID: 19332369
- An evaluation of chemical photoreactivity and the relationship to photogenotoxicity. | Lynch, AM., et al. 2010. Regul Toxicol Pharmacol. 58: 219-23. PMID: 19914326
- An evaluation of chemical photoreactivity and the relationship to phototoxicity. | Kleinman, MH., et al. 2010. Regul Toxicol Pharmacol. 58: 224-32. PMID: 20600453
- EP4 receptor as a new target for bronchodilator therapy. | Buckley, J., et al. 2011. Thorax. 66: 1029-35. PMID: 21606476
- Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists. | Allan, AC., et al. 2011. Bioorg Med Chem Lett. 21: 4343-8. PMID: 21676612
- Reciprocal regulation of NADPH oxidases and the cyclooxygenase-2 pathway. | Sancho, P., et al. 2011. Free Radic Biol Med. 51: 1789-98. PMID: 21907277
- EP4 receptors mediate prostaglandin E2, tumour necrosis factor alpha and interleukin 1beta-induced ion secretion in human and mouse colon mucosa. | Fairbrother, SE., et al. 2012. Eur J Pharmacol. 694: 89-97. PMID: 22732652
- Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor. | Birrell, MA., et al. 2013. Br J Pharmacol. 168: 129-38. PMID: 22747912
- Prostanoid receptors mediating contraction in rat, macaque and human bladder smooth muscle in vitro. | Root, JA., et al. 2015. Eur J Pharmacol. 769: 274-9. PMID: 26607459
- Curcumin Ameliorates the Reduction Effect of PGE2 on Fibrillar β-Amyloid Peptide (1-42)-Induced Microglial Phagocytosis through the Inhibition of EP2-PKA Signaling in N9 Microglial Cells. | He, GL., et al. 2016. PLoS One. 11: e0147721. PMID: 26824354
- Inhibition of STAT3- and MAPK-dependent PGE2 synthesis ameliorates phagocytosis of fibrillar β-amyloid peptide (1-42) via EP2 receptor in EMF-stimulated N9 microglial cells. | He, GL., et al. 2016. J Neuroinflammation. 13: 296. PMID: 27871289
- Tuberin Regulates Prostaglandin Receptor-Mediated Viability, via Rheb, in mTORC1-Hyperactive Cells. | Li, C., et al. 2017. Mol Cancer Res. 15: 1318-1330. PMID: 28710231
Inhibitor of:
EP1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GW 848687X, 500 µg | sc-295034 | 500 µg | $147.00 | |||
GW 848687X, 1 mg | sc-295034A | 1 mg | $279.00 |