L-161,982

Names

[ Name ]:
L-161,982

[Synonym ]:
L-161,982
HMS3269M17
Peroxy Orange 1

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

Research Areas >> Inflammation/Immunology

[Target]

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.

[References]

[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.

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.37g/cm3

[ Melting Point ]:
> 145 °C

[ Molecular Formula ]:
C₃₂H₂₉F₃N₄O₄S₂

[ Molecular Weight ]:
654.72200

[ Exact Mass ]:
654.15800

[ PSA ]:
139.68000

[ LogP ]:
8.07100

[ Index of Refraction ]:
1.633

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

Systemic EP4 Inhibition Increases Adhesion Formation in a Murine Model of Flexor Tendon Repair.

PLoS ONE 10 , e0136351, (2015)

Flexor tendon injuries are a common clinical problem, and repairs are frequently complicated by post-operative adhesions forming between the tendon and surrounding soft tissue. Prostaglandin E2 and th...