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MF498 (CAS 915191-42-3) LS-H121

EP4 receptor antagonist
LS-H121-1 / 1 mg / $195
LS-H121-5 / 5 mg / $335
LS-H121-10 / 10 mg / $465
LS-H121-25 / 25 mg / $1005
USA Shipment Only
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Description: Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis. MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors). In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM. In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day). H121_ChemicalStructureImage.png
biochemical, chemical, antagonist
A crystalline solid
Shipped at 4°C, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: PTGER4 / EP4 related products

Usage Information

MF498 is supplied as a crystalline solid. A stock solution may be made by dissolving the MF498 in the solvent of choice. MF498 is soluble in organic solvents such as DMSO and dimethyl formamide, which should be purged with an inert gas. The solubility of MF498 in these solvents is approximately 10 mg/ml. MF498 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, MF498 should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. MF498 has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

  1. Li, M., Thompson, D.D., and Paralkar, V.M. Prostaglandin E2 receptors in bone formation. Int. Orthop. 31, 767-772 (2007).
  2. Hawcroft, G., Ko, C.W.S., and Hull, M.A. Prostaglandin E2-EP4 receptor signalling promotes tumorigenic behaviour of HT-29 human colorectal cancer cells. Oncogene 26, 3006-3019 (2007).
  3. Babaev, V.R., Chew, J.D., Ding, L., et al. Macrophage EP4 deficiency increases apoptosis and suppresses early atherosclerosis. Cell Metab. 8, 492-501 (2008).
  4. Clark, P., Rowland, S.E., Denis, D., et al. MF498 [N-{[4-(5,9-diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin- 7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis. J. Pharmacol. Exp. Ther. 325(2), 425- 434 (2008).


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