KAG-308
Based on 3 publication(s) in Google Scholar
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor.
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- Purity : 98.62%
- CAS No.: 1215192-68-9
- 화학식: C24H30F2N4O3
- 분자량:460.52
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보관:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) KAG-308
More
Biological Activity
제품 설명
IC50 & Target
EC50: 17 nM (Human EP4 receptor), 160 nM (Human EP3 receptor), 1000 nM (Human EP2 receptor), 1000 nM (Human EP2 receptor)[1]
Ki: 2.57 nM (Human EP4 receptor), 32.4 nM (Human EP3 receptor), 52.9 nM (Human IP receptor), 1410 nM (Human EP1 receptor), 1540 nM (Human EP2 receptor)[1]
In Vitro
KAG-308 is a potent selective and orally active agonist of EP4 receptor, suppresses colitis and promots histological mucosal healing. KAG-308 shows a Ki and EC50 values of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over human EP1 (Ki, 1410 nM; EC50, 1000 nM), EP2 (Ki, 1540 nM; EC50, 1000 nM), EP3 (Ki, 32.4 nM; EC50, 160 nM) and IP receptor (Ki, 52.9 nM; EC50, >10000 nM). KAG-308 also exhibits potent agonist activity for human and mouse EP4 with an EC50 of 0.15 nM and 1.0 nM, respectively in the dual luciferase reporter assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1215192-68-9
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Appearance Solid
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분자량 460.52
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화학식 C24H30F2N4O3
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Color White to light yellow
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SMILES
O[C@H](C1)[C@H](/C=C/[C@@H](O)[C@@H](C2=CC=CC(C)=C2)C)[C@](C/3(F)F)([H])[C@@]1([H])OC3=C/CCCC4=NN=NN4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell
2025 Dec 11;188(25):7291-7308.e23. PMID: 41161316 -
Cancer Discov
Tumor-Derived Lysophosphatidic Acid Blunts Protective Type I Interferon Responses in Ovarian Cancer. [Abstract]2022 Aug 5;12(8):1904-1921. PMID: 35552618 -
In Vitro Cell Dev Biol Anim
Atorvastatin inhibits ischemia‒reperfusion-associated renal tubular cell ferroptosis by blocking the PGE2/EP4 signaling pathway. [Abstract]2025 Mar;61(3):275-287. PMID: 39920560
용액&용해도
In Vitro:
DMSO : 80 mg/mL (173.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 6 mg/mL (13.03 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 6 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 6 mg/mL (13.03 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 6 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 (60.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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DSS-Induced Colitis
Dextran sulfate sodium (DSS)-induced colitis is generated by administering DSS in mouse drinking water, producing epithelial injury, barrier disruption, weight loss, diarrhea, fecal blood, colon shortening, histologic mucosal damage, and inflammatory mediator changes; the model is mainly used to study acute or chronic intestinal inflammation resembling selected features of ulcerative colitis. DSS injury is interpreted through clinical and tissue readouts rather than a single molecular endpoint: daily body weight, stool consistency, and bleeding are combined into a disease activity index, while colon length, histology, cytokines, myeloperoxidase activity, intestinal permeability, and tight-junction markers provide complementary measures of inflammation and barrier damage.
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TNBS-Induced Colitis
TNBS-induced colitis is produced by intrarectal delivery of 2,4,6-trinitrobenzene sulfonic acid in ethanol, where ethanol disrupts the mucosal barrier and TNBS haptenates colonic proteins, generating immune-mediated colonic inflammation with weight loss, diarrhea, ulceration, transmural injury, inflammatory-cell infiltration, and cytokine responses. The model is used as an experimental intestinal inflammation model with Crohn’s disease–like features, especially when Th1-type responses, IL-12–dependent inflammation, chronic relapsing inflammation, or fibrosis-related endpoints are studied.
순도&문서
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1715 mL | 10.8573 mL | 21.7146 mL | 54.2865 mL |
| 5 mM | 0.4343 mL | 2.1715 mL | 4.3429 mL | 10.8573 mL | |
| 10 mM | 0.2171 mL | 1.0857 mL | 2.1715 mL | 5.4286 mL | |
| 15 mM | 0.1448 mL | 0.7238 mL | 1.4476 mL | 3.6191 mL | |
| 20 mM | 0.1086 mL | 0.5429 mL | 1.0857 mL | 2.7143 mL | |
| 25 mM | 0.0869 mL | 0.4343 mL | 0.8686 mL | 2.1715 mL | |
| 30 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8095 mL | |
| 40 mM | 0.0543 mL | 0.2714 mL | 0.5429 mL | 1.3572 mL | |
| 50 mM | 0.0434 mL | 0.2171 mL | 0.4343 mL | 1.0857 mL | |
| 60 mM | 0.0362 mL | 0.1810 mL | 0.3619 mL | 0.9048 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6786 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5429 mL |
KAG-308 Related Classifications
HY-128686 Related Classifications
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