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

L-161982 

Cat. No.: HY-108559
Handling Instructions

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

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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].

IC50 & Target[1]

EP4

 

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].

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].

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.

147776-06-5

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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

L-161982L161982L 161982Prostaglandin ReceptorprostaglandinproliferationcoloncancerarthritisphosphorylationInhibitorinhibitorinhibit

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L-161982
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