1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. L-161982

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.

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

L-161982 Chemical Structure

L-161982 Chemical Structure

CAS No. : 147776-06-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 360 In-stock
Solution
10 mM * 1 mL in DMSO USD 360 In-stock
Solid
1 mg USD 90 In-stock
5 mg USD 250 In-stock
10 mg USD 390 In-stock
25 mg USD 690 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: HCA-7 cells
Concentration: 10 μM
Incubation Time: 2 hours
Result: Blocked PGE2-induced cell proliferation.
In Vivo

L-161982 (5 mg/kg; i.p.; once per day for 2 weeks) reduces arthritis lesions and lesion progression in CIA mice[2].

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

Animal Model: Female DBA/1 mice of 6 to 8 weeks old (collagen-induced arthritis (CIA) mice model)[1]
Dosage: 5 mg/kg
Administration: i.p.; once per day for 2 weeks
Result: Showed less joint swelling and lower arthritis score after 35 days post immunization.
Molecular Weight

654.72

Formula

C32H29F3N4O4S2

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5274 mL 7.6369 mL 15.2737 mL
5 mM 0.3055 mL 1.5274 mL 3.0547 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, 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.

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  • Dilution Calculator

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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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
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. 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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L-161982 Related Classifications

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  • 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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L-161982
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