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CJ-42794

Catalog No. T14975   CAS 847728-01-2
Synonyms: CJ-042794

CJ-42794 (CJ-042794) is a selective antagonist of prostaglandin E receptor subtype 4 (EP4). It inhibits [3H]-PGE2 binding to the human EP4 receptor (a mean pKi: 8.5). CJ-42794 is a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3) (IC50 : 8.5 (pKi )).

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CJ-42794 Chemical Structure
CJ-42794, CAS 847728-01-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 32.00
10 mg In stock $ 50.00
25 mg In stock $ 98.00
1 mL * 10 mM (in DMSO) In stock $ 51.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CJ-42794 (CJ-042794) is a selective antagonist of prostaglandin E receptor subtype 4 (EP4). It inhibits [3H]-PGE2 binding to the human EP4 receptor (a mean pKi: 8.5). CJ-42794 is a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3) (IC50 : 8.5 (pKi )).
In vitro CJ-042794 competitively inhibits PGE2-evoked elevations of intracellular cAMP levels in HEK293 cells overexpressing human EP4receptor (mean pA2: 8.6). CJ-042794 reverses the inhibitory effects of PGE2 on LPS-induced TNFα production in a concentration-dependent manner [1].
In vivo CJ-42794 significantly delays ulcer healing in rats and mice and these responses were both attenuated by coadministration of CJ-42794 [2].
Synonyms CJ-042794
Molecular Weight 413.83
Formula C22H17ClFNO4
CAS No. 847728-01-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 28 mg/mL (67.66 mM)

TargetMolReferences and Literature

1. Murase A, et al. In vitro pharmacological characterization of CJ-042794, a novel, potent, and selective prostaglandin EP(4) receptor antagonist. Life Sci. 2008 Jan 16;82(3-4):226-232. 2. Hatazawa R, et al. Cyclooxygenase-2/prostaglandin E2 accelerates the healing of gastric ulcers via EP4 receptors. Am J Physiol Gastrointest Liver Physiol. 2007 Oct;293(4):G788-97.

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Keywords

CJ-42794 847728-01-2 Others prostaglandin E2 CJ42794 tumor necrosis factor α CJ042794 cAMP gastric ulcers NR3C3 inhibit CJ 42794 human whole blood CJ 042794 Progesterone Receptor Inhibitor CJ-042794 inhibitor

 

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