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847728-01-2

847728-01-2 structure
847728-01-2 structure
  • Name: CJ-42794
  • Chemical Name: 4-[(1S)-1-[[5-chloro-2-(4-fluorophenoxy)benzoyl]amino]ethyl]benzoic acid
  • CAS Number: 847728-01-2
  • Molecular Formula: C22H17ClFNO4
  • Molecular Weight: 413.826
  • Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
  • Create Date: 2018-12-23 17:24:26
  • Modify Date: 2024-01-09 21:02:58
  • CJ-42794 is a selective prostaglandin E receptor subtype 4(EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, 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 value: 8.5 (pKi ) [1]Target: EP4in vitro: CJ-042794 competitively inhibits PGE2-evoked elevations of intracellular cAMP levels in HEK293 cells overexpressing human EP4receptor with a mean pA2 value of 8.6. PGE2 inhibits the lipopolysaccharide (LPS)-induced production of tumor necrosis factor α (TNFα) in human whole blood (HWB); 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 the ulcer healing in rats and mice. The expression of VEGF in primary rat gastric fibroblasts was increased by PGE2 or AE1-329 (EP4 agonist), and these responses were both attenuated by coadministration of CJ-42794.[2]

Name 4-[(1S)-1-[[5-chloro-2-(4-fluorophenoxy)benzoyl]amino]ethyl]benzoic acid
Synonyms (S)-4-(1-(5-chloro-2-(4-fluorophenoxy)benzamido)ethyl)benzoic acid
4-[(1S)-1-{[5-Chloro-2-(4-fluorophenoxy)benzoyl]amino}ethyl]benzoic acid
Benzoic acid, 4-[(1S)-1-[[5-chloro-2-(4-fluorophenoxy)benzoyl]amino]ethyl]-
CJ-42794
Description CJ-42794 is a selective prostaglandin E receptor subtype 4(EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, 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 value: 8.5 (pKi ) [1]Target: EP4in vitro: CJ-042794 competitively inhibits PGE2-evoked elevations of intracellular cAMP levels in HEK293 cells overexpressing human EP4receptor with a mean pA2 value of 8.6. PGE2 inhibits the lipopolysaccharide (LPS)-induced production of tumor necrosis factor α (TNFα) in human whole blood (HWB); 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 the ulcer healing in rats and mice. The expression of VEGF in primary rat gastric fibroblasts was increased by PGE2 or AE1-329 (EP4 agonist), and these responses were both attenuated by coadministration of CJ-42794.[2]
Related Catalog
References

[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.

Density 1.3±0.1 g/cm3
Boiling Point 572.7±50.0 °C at 760 mmHg
Molecular Formula C22H17ClFNO4
Molecular Weight 413.826
Flash Point 300.2±30.1 °C
Exact Mass 413.083008
PSA 75.63000
LogP 5.91
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.616
Storage condition 2-8℃
HS Code 2924299090
HS Code 2924299090
Summary 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%