L-161982
Based on 1 publication(s) in Google Scholar
L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice.
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- Pureté: 99.33%
- CAS No.: 147776-06-5
- Formule: C32H29F3N4O4S2
- Masse moléculaire:654.72
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) L-161982
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Activité biologique
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EP4 |
L-161982 (10 μM; 2 hours) blocks PGE2-stimulated cell proliferation of HCA-7 cells[1].
L-161982 (10 μM; 1 hour) blocks PGE2-stimulated ERK phosphorylation in HCA-7 cells[1].
L-161982 induces apoptosis, cell cycle arrest, and inhibits prostaglandin E2-induced proliferation in oral squamous carcinoma Tca8113 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCA-7 cells
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Concentration:10 μM
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Incubation Time:2 hours
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Result:Blocked PGE2-induced cell proliferation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female DBA/1 mice of 6 to 8 weeks old (collagen-induced arthritis (CIA) mice model)[1]
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Dosage:5 mg/kg
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Administration:i.p.; once per day for 2 weeks
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Result:Showed less joint swelling and lower arthritis score after 35 days post immunization.
Chemical Information
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CAS No. 147776-06-5
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Appearance Solid
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Masse moléculaire 654.72
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Formule C32H29F3N4O4S2
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Color White to off-white
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SMILES
O=C(C1=C(C)C=CS1)NS(=O)(C2=CC=CC=C2C3=CC=C(CN4C(CCCC)=NN(C5=CC=CC=C5C(F)(F)F)C4=O)C=C3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Ann Rheum Dis
2025 Oct 28:S0003-4967(25)04428-0. PMID: 41162285
Solvant et solubilité
DMSO : 100 mg/mL (152.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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)
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.
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.
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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Li X, et al.The EP4 antagonist, L-161,982, induces apoptosis, cell cycle arrest, and inhibits prostaglandin E2-induced proliferation in oral squamous carcinoma Tca8113 cells.J Oral Pathol Med. 2017 Nov;46(10):991-997. [Content Brief]
[2]. Cherukuri DP, et al. The EP4 receptor antagonist, L-161,982, blocks prostaglandin E2-induced signal transduction and cell proliferation in HCA-7 colon cancer cells.Exp Cell Res. 2007 Aug 15;313(14):2969-79. [Content Brief]
[3]. Chen L, et al. L161982 alleviates collagen-induced arthritis in mice by increasing Treg cells and down-regulating Interleukin-17 and monocyte-chemoattractant protein-1 levels.BMC Musculoskelet Disord. 2017 Nov 16;18(1):462. [Content Brief]
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. 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 | 1.5274 mL | 7.6369 mL | 15.2737 mL | 38.1843 mL |
| 5 mM | 0.3055 mL | 1.5274 mL | 3.0547 mL | 7.6369 mL | |
| 10 mM | 0.1527 mL | 0.7637 mL | 1.5274 mL | 3.8184 mL | |
| 15 mM | 0.1018 mL | 0.5091 mL | 1.0182 mL | 2.5456 mL | |
| 20 mM | 0.0764 mL | 0.3818 mL | 0.7637 mL | 1.9092 mL | |
| 25 mM | 0.0611 mL | 0.3055 mL | 0.6109 mL | 1.5274 mL | |
| 30 mM | 0.0509 mL | 0.2546 mL | 0.5091 mL | 1.2728 mL | |
| 40 mM | 0.0382 mL | 0.1909 mL | 0.3818 mL | 0.9546 mL | |
| 50 mM | 0.0305 mL | 0.1527 mL | 0.3055 mL | 0.7637 mL | |
| 60 mM | 0.0255 mL | 0.1273 mL | 0.2546 mL | 0.6364 mL | |
| 80 mM | 0.0191 mL | 0.0955 mL | 0.1909 mL | 0.4773 mL | |
| 100 mM | 0.0153 mL | 0.0764 mL | 0.1527 mL | 0.3818 mL |
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