CJ-42794
- Product Name
- CJ-42794
- CAS No.
- 847728-01-2
- Chemical Name
- CJ-42794
- Synonyms
- CJ-42794;CJ-042794;RQ-00015986;CJ-042794 (CJ-042794);CJ-42794, 10 mM in DMSO;CJ-042794;CJ42794;CJ 42794;4-((S)-1-(2-(4-fluorophenoxy)-5-chlorobenzamido)ethyl)benzoic acid;(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]-
- CBNumber
- CB52473902
- Molecular Formula
- C22H17ClFNO4
- Formula Weight
- 413.83
- MOL File
- 847728-01-2.mol
CJ-42794 Property
- 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
- form
- A crystalline solid
- pka
- 4.21±0.10(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H317May cause an allergic skin reaction
H319Causes serious eye irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P272Contaminated work clothing should not be allowed out of the workplace.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P363Wash contaminated clothing before reuse.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 10010428
- Product name
- CJ-42794
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $53
- Updated
- 2024/03/01
- Product number
- 10010428
- Product name
- CJ-42794
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $227
- Updated
- 2024/03/01
- Product number
- 10010428
- Product name
- CJ-42794
- Purity
- ≥98%
- Packaging
- 100mg
- Price
- $399
- Updated
- 2024/03/01
- Product number
- 10010428
- Product name
- CJ-42794
- Purity
- ≥98%
- Packaging
- 250mg
- Price
- $747
- Updated
- 2024/03/01
- Product number
- 095360
- Product name
- (S)-4-(1-(5-Chloro-2-(4-fluorophenoxy)-benzamido)ethyl)benzoic acid
- Purity
- 95+%
- Packaging
- 1g
- Price
- $750
- Updated
- 2021/12/16
CJ-42794 Chemical Properties,Usage,Production
Uses
CJ-42794 (CJ-042794) is a potent, orally active, selective prostaglandin E receptor 4 (EP4) antagonist with an IC50 value of 10 nM, which is 200-fold more selective than EP1, EP2 and EP3. CJ-42794 can be used in research of gastric ulcers[1][2].
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].
IC 50
EP: 10 nM (EC50)
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.
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