CJ-42794
- CAS NO.:847728-01-2
- Empirical Formula: C22H17ClFNO4
- Molecular Weight: 413.83
- MDL number: MFCD13184815
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-13 11:39:26
What is CJ-42794?
Definition
ChEBI: Benzoic acid, 4-[(1s)-1-[[5-chloro-2-(4-fluorophenoxy)benzoyl]amino]ethyl]- is an aromatic ether.
Biological Activity
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.
Properties of CJ-42794
Boiling point: | 572.7±50.0 °C(Predicted) |
Density | 1.347±0.06 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | insoluble in H2O; ≥11.7 mg/mL in DMSO; ≥54.6 mg/mL in EtOH |
pka | 4.21±0.10(Predicted) |
form | A crystalline solid |
color | White to off-white |
Safety information for CJ-42794
Computed Descriptors for CJ-42794
New Products
(R)-3-Aminobutanenitrile Hydrochloride 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION AMOXICILLIN (AMOXYCILLIN) TRIHYDRATE ACICLOVIR AMLODIPINE SODIUM METHYL PARABEN Methylcobalamin (vitamin B12) SODIUM VALPROATE 5-Fluoro-2-iodo-3-methylaniline Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 1-Methyl-6-oxo-1,6-dihydropyridazine-3-carbonitrile 3-Bromo-2-hydroxybenzeneacetic acid 5-Iodo-3-methyl-2-nitropyridine 1-(3-Chloro-2-hydroxyphenyl)-2-propanoneRelated products of tetrahydrofuran
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