An EP4 receptor antagonist
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CJ-023423

Item No. 10010355

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[2,4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenylethylamino]carbonyl]-4-methyl-benzenesulfonamide
CAS Number
415903-37-6
Synonyms
  • Grapiprant
  • RQ-00000007
Molecular Formula
C26H29N5O3S
Formula Weight
491.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
SMILES
O=C(NS(C1=CC=C(C)C=C1)(=O)=O)NCCC2=CC=C(N3C(CC)=NC4=C(C)N=C(C)C=C43)C=C2
InChi Code
InChI=1S/C26H29N5O3S/c1-5-24-29-25-19(4)28-18(3)16-23(25)31(24)21-10-8-20(9-11-21)14-15-27-26(32)30-35(33,34)22-12-6-17(2)7-13-22/h6-13,16H,5,14-15H2,1-4H3,(H2,27,30,32)
InChi Key
HZVLFTCYCLXTGV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Product 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, cancer, and atherosclerosis.1,2,3 CJ-023423 is a potent and selective antagonist of the EP4 receptor (Ki = 13 and 20 nM for human and rat EP4, respectively).4,5 It inhibits PGE2-evoked elevation in intracellular cAMP in cells and, in vivo, reduces thermal hyperalgesia induced by intraplantar injection of PGE2.4 CJ-023423 reduces acute and chronic inflammatory pain in different mouse models.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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).

    2. Li, M., Thompson, D.D., and Paralkar, V.M. Prostaglandin E2 receptors in bone formation. Int. Orthop. 31(6), 767-772 (2007).

    3. 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).

    4. Nakao, K., Murase, A., Ohshiro, H., et al. CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. J. Pharmacol. Exp. Ther. 322(2), 686-694 (2007).

    5. Jones, R.L., Giembycz, M.A., and Woodward, D.F. Prostanoid receptor antagonists: Development strategies and therapeutic applications. Br. J. Pharmacol. 158(1), 104-145 (2009).