| Bioactivity | 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]. | ||||||||||||
| Invitro | 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: | ||||||||||||
| 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: | ||||||||||||
| Name | L-161982 | ||||||||||||
| CAS | 147776-06-5 | ||||||||||||
| Formula | C32H29F3N4O4S2 | ||||||||||||
| Molar Mass | 654.72 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |