A selective EP4 antagonist
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MF498

Item No. 15973

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[[4-(5,9-diethoxy-6,8-dihydro-6-oxo-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylphenyl]methyl]sulfonyl]-2-methoxy-benzeneacetamide
CAS Number
915191-42-3
Molecular Formula
C32H33N3O7S
Formula Weight
603.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 20 mg/mlEthanol:PBS (pH 7.2) (1:1): 0.09 mg/ml
λmax
204, 255 nm
SMILES
O=C1N(C2=C(C)C=C(CS(NC(CC3=CC=CC=C3OC)=O)(=O)=O)C=C2)CC4=C(OCC)C5=C(C=CC=N5)C(OCC)=C41
InChi Code
InChI=1S/C32H33N3O7S/c1-5-41-30-23-11-9-15-33-29(23)31(42-6-2)24-18-35(32(37)28(24)30)25-14-13-21(16-20(25)3)19-43(38,39)34-27(36)17-22-10-7-8-12-26(22)40-4/h7-16H,5-6,17-19H2,1-4H3,(H,34,36)
InChi Key
WVLIUERFVJYBNY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $75

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    10 mg

    $589

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    25 mg

    $1,286

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    Product Description

    Prostaglandin E2 (PGE2; Item No. 14010) 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.1,2,3 MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).4 In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.4 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).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, M., Thompson, D.D., and Paralkar, V.M. Prostaglandin E2 receptors in bone formation. Int. Orthop. 31(6), 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(21), 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(6), 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).