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CJ-42794

Cat. No. M10807
CJ-42794 Structure
Synonym:

CJ-042794

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Biological Activity

CJ-42794 is a selective prostaglandin receptor EP4 antagonist that inhibits [3H]-PGE2 binding to EP4 receptors with an average pKi of 8.5 and is more than 200 times more selective than EP1, EP2 and EP3.

Chemical Information
Molecular Weight 413.83
Formula C22H17ClFNO4
CAS Number 847728-01-2
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Al Mamun, et al. Physiol Rep. A selective antagonist of prostaglandin E receptor subtype 4 attenuates abdominal aortic aneurysm

[2] Zhengxing Zhang, et al. Bioorg Med Chem Lett. Synthesis and evaluation of 18 F-labeled CJ-042794 for imaging prostanoid EP4 receptor expression in cancer with positron emission tomography

[3] Akio Murase, et al. Life Sci. In vitro pharmacological characterization of CJ-042794, a novel, potent, and selective prostaglandin EP(4) receptor antagonist

[4] Ryo Hatazawa, et al. Am J Physiol Gastrointest Liver Physiol. Cyclooxygenase-2/prostaglandin E2 accelerates the healing of gastric ulcers via EP4 receptors

[5] Koji Takeuchi, et al. J Pharmacol Exp Ther. Effect of (S)-4-(1-(5-chloro-2-(4-fluorophenyoxy)benzamido)ethyl) benzoic acid (CJ-42794), a selective antagonist of prostaglandin E receptor subtype 4, on ulcerogenic and healing responses in rat gastrointestinal mucosa

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Keywords: CJ-42794, CJ-042794 supplier, Prostaglandin Receptor, inhibitors, activators


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