1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. CJ-42794

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.

For research use only. We do not sell to patients.

CJ-42794 Chemical Structure

CJ-42794 Chemical Structure

CAS No. : 847728-01-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 60 In-stock
50 mg USD 204 In-stock
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE CJ-42794

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target

EP

10 nM (EC50)

In Vitro

CJ-042794 (CJ-042794, 0.3-5000 nM; 10 min; hEP4/HEK293 cells) inhibits the PGE2-induced elevation of cAMP in a concentration-dependent manner with a pIC50 value of 7.5[1].
CJ-042794 (3-3000 nM; 24 h) reverses the inhibitory effects of PGE2 (10 nM) on the LPS-induced TNFα production in human whole blood (HWB) in a concentration-dependent manner with a pIC50 value of 6.4[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CJ-042794 (CJ-042794; 0.3-3 mg/kg; i.d.; once) antagonizes the HCO3 stimulatory action of AE1-329 in the duodenum[1].
CJ-042794 (30 and 50 mg/kg; p.o.; once) does not cause any damage to the gastric mucosa of normal rats and has no gastric ulcerogenic response to cold-restraint stress[1].
CJ-042794 (30 and 50 mg/kg; p.o.; once) does not damage the stomach and small intestine of helper arthritis rats[1].
CJ-042794 (3-45 mg/kg; p.o.; twice daily for 14 d; Sprague-Dawley rats) promotes spontaneous healing of gastric ulcers[1].
CJ-042794 (10 mg/kg; p.o.; daily, for 7 d) repeats administration impairs the healing of chronic gastric ulcers with a down-regulation of vascular endothelial growth factor expression in the ulcerated mucosa[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (200-230 g)[1]
Dosage: 0.3, 1, and 3 mg/kg
Administration: intradermal injection; once
Result: Attenuated the PGE2-stimulated HCO3 secretion in a dose-dependent manner and had the inhibition being 68.9% at 1 mg/kg.
Animal Model: Male Sprague-Dawley rats (200-230 g)[1]
Dosage: 30 and 50 mg/kg
Administration: Oral administration; once
Result: Did not produce any damage in the gastrointestinal mucosa.
Did not produce gastric ulcerogenic response induced by cold-restraint stress.
Animal Model: Dark Agouti (DA) rats (140-160 g)[1]
Dosage: 30 and 50 mg/kg
Administration: Oral administration; once
Result: Caused any visible damage in the gastric mucosa of normal rats.
Had little injurious effect on the small intestine of arthritic rats.
Animal Model: Male Sprague-Dawley rats (200-230 g)[1]
Dosage: 3, 10, and 45 mg/kg
Administration: Oral administration; twice daily for 14 days
Result: Healed ulcers gradually within 14 days, and the ulcer score on day 17 was 1.6 mm2.
Animal Model: Male Sprague-Dawley rats (200-230 g)[1]
Dosage: 10 mg/kg
Administration: Oral administration; daily for 7 days
Result: Down-regulates the expression of VEGF and decreased the angiogenic response.
Molecular Weight

413.83

Formula

C22H17ClFNO4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(OC2=CC=C(F)C=C2)C(C(N[C@H](C3=CC=C(C(O)=O)C=C3)C)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (67.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4165 mL 12.0823 mL 24.1645 mL
5 mM 0.4833 mL 2.4165 mL 4.8329 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.04 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.84%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4165 mL 12.0823 mL 24.1645 mL 60.4113 mL
5 mM 0.4833 mL 2.4165 mL 4.8329 mL 12.0823 mL
10 mM 0.2416 mL 1.2082 mL 2.4165 mL 6.0411 mL
15 mM 0.1611 mL 0.8055 mL 1.6110 mL 4.0274 mL
20 mM 0.1208 mL 0.6041 mL 1.2082 mL 3.0206 mL
25 mM 0.0967 mL 0.4833 mL 0.9666 mL 2.4165 mL
30 mM 0.0805 mL 0.4027 mL 0.8055 mL 2.0137 mL
40 mM 0.0604 mL 0.3021 mL 0.6041 mL 1.5103 mL
50 mM 0.0483 mL 0.2416 mL 0.4833 mL 1.2082 mL
60 mM 0.0403 mL 0.2014 mL 0.4027 mL 1.0069 mL
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CJ-42794 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CJ-42794
Cat. No.:
HY-10797
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