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CJ-42794

Catalog No.
C4037
EP4 antagonist
Grouped product items
SizePriceStock Qty
50mg
$269.00
Ship with 5-10 days
100mg
$478.00
Ship with 5-10 days
250mg
$896.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Ki: 3.16 nM: antagonizes E prostanoid receptor 4 (EP4).

Ki: 631 nM: antagonizes EP2.

CJ-42794, as a selective antagonist of EP4, less binds to EP2 and does not have binding affinity for EP1 or EP3. It displays minimal effect on numerous other receptors, channels, or enzymes. CJ-42794 delays the healing of gastric ulcers, inhibiting the upregulation of VEGF expression and angiogenesis. EP4, activated by prostaglandin E2 (PGE2), is a G-protein-coupled receptor, which plays vital roles in bone formation and resorption, cancer, and atherosclerosis via elevating the second messenger cyclic AMP (cAMP).

In vitro: CJ-42794 exhibited remarkable binding activity to EP4 and suppressed PGE2-triggered elevations of intracellular cAMP levels in a concentration-dependent fashion in HEK293 cells overexpressing human EP4. Moreover, CJ-42794, concentration-dependently, reversed the inhibitory effects of PGE2 on lipopolysaccharide-evoked tumor necrosis factor α production, which suggested that CJ-42794 had excellent pharmacological properties used for exploring the physiological role of EP4 [1].

In vivo: Male Sprague-Dawley rats and C57BL/6 mice were given subcutaneously 3 and 10 mg/kg for rats, 10 mg/kg for mice once daily for 7 or 14 days. Compared to the controls, CJ-42794, in a dose-dependent manner, impaired and delayed the gastric ulcer healing in rats and mice. CJ-42794 markedly dampened the increase of VEGF expression in ulcerated mucosa of the mouse stomach and the primary gastric fibroblasts of rat [2].

References:
[1].  Murase, A., Taniguchi, Y., Tonai-Kachi, H., Nakao, K., & Takada, J. In vitro pharmacological characterization of CJ-042794, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Life Sciences. 2008; 82(3-4): 226-232.
[2].  Hatazawa, R., Tanaka, A., Tanigami, M., Amagase, K., Kato, S., Ashida, Y., & Takeuchi, K. Cyclooxygenase-2/prostaglandin E2 accelerates the healing of gastric ulcers via EP4 receptors. AJP: Gastrointestinal and Liver Physiology. 2007; 293(4): G788-G797.

Chemical Properties

StorageStore at -20°C
M.Wt413.8
Cas No.847728-01-2
FormulaC22H17ClFNO4
SynonymsRQ-00015986
Solubilityinsoluble in H2O; ≥11.7 mg/mL in DMSO; ≥54.6 mg/mL in EtOH
Chemical Name4-[(1S)-1-[[5-chloro-2-(4-fluorophenoxy)benzoyl]amino]ethyl]-benzoic acid
SDFDownload SDF
Canonical SMILESFC1=CC=C(OC2=C(C(N[[email protected]@H](C)C3=CC=C(C(O)=O)C=C3)=O)C=C(Cl)C=C2)C=C1
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

CJ-42794